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https://en.wikipedia.org/wiki/GPR31 | G-protein coupled receptor 31 also known as 12-(S)-HETE receptor is a protein that in humans is encoded by the GPR31 gene. The human gene is located on chromosome 6q27 and encodes a G-protein coupled receptor protein composed of 319 amino acids.
Function
The GPR31 receptor is most closely related in amino acid sequence to the oxoeicosanoid receptor 1, a G-protein coupled receptor encoded by the GPR170 gene. Oxoeicosanoid receptor 1 is the receptor for a family of arachidonic acid metabolites made by 5-lipoxygenase viz., 5-Hydroxyicosatetraenoic acid (5-HETE), 5-oxoicosanoic acid (5-oxo-ETE) and other members of this family of broadly bioactive cell stimuli. The GPR31 receptor is a receptor for very different arachidonic acid metabolite, 12-hydroxyeicosatetraenoic acid (12-HETE), whose synthesis is catalyzed by 12-lipoxygenase; this conclusion is based on studies that cloned the receptor from the PC-3 prostate cancer cell line and found that the cloned receptor, when expressed in other cell types, bound with high affinity (Kd=5 nM) and mediated the actions of low concentrations of the S but not R stereoisomer of 12-HETE. In a [35S]GTPγS binding assay, which indirectly estimates a receptor's binding affinity with a ligand by measuring this ligand's ability to stimulate the receptor to bind [35S]GTPγS, 12(S)-HETE stimulated the cloned GPR31 receptor to bind [35S]GTPγS with an EC50 (effective concentration causing a 50% of maximal rise in [35S]GTPγS binding) was <0.3 nM; it |
https://en.wikipedia.org/wiki/GPR32 | G protein-coupled receptor 32, also known as GPR32 or the RvD1 receptor, is a human receptor (biochemistry) belonging to the rhodopsin-like subfamily of G protein-coupled receptors.
Gene
The GPR32 was initially identified and defined by molecular cloning in 1998 as coding for an orphan receptor, i.e. a protein with an amino acid sequence similar to known receptors but having no known ligand(s) to which it responds and no known function. The projected amino acid sequence of GPR32, however, shared 35-39% amino acid identity with certain members of the chemotactic factor receptor family, i.e. 39% identity with Formyl peptide receptor 1, which is a receptor for N-Formylmethionine-leucyl-phenylalanine and related N-formyl peptide chemotactic factors, and 35% identity with Formyl peptide receptor 2, which likewise is also a receptor for N-formyl peptides but also a receptor for certain lipoxins which are arachidonic acid metabolites belonging to a set of specialized proresolving mediators that act to resolve or inhibit inflammatory reactions. GPR32 mapped to chromosomal 19, region q13.3. There are no mouse or other orthologs of GPR32.
Receptor
The GPR32 protein is a G protein coupled receptor although the specific G protein subtypes which it activates has not yet been reported. GPR32 is expressed in human blood neutrophils, certain types of blood lymphocytes (i.e. activated CD8+ cells, CD4+ T cells, and T helper 17 cells), tissue macrophages, small airway epithelial cells, and |
https://en.wikipedia.org/wiki/GPR33 | Probable G-protein coupled receptor 33 is a protein that in humans is encoded by the GPR33 gene.
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR34 | Probable G-protein coupled receptor 34 is a protein that in humans is encoded by the GPR34 gene.
Function
G protein-coupled receptors (GPCRs), such as GPR34, are integral membrane proteins containing 7 putative transmembrane domains (TMs). These proteins mediate signals to the interior of the cell via activation of heterotrimeric G proteins that in turn activate various effector proteins, ultimately resulting in a physiologic response.[supplied by OMIM]
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR37 | Probable G-protein coupled receptor 37 is a protein that in humans is encoded by the GPR37 gene. GPR37 is primarily found in the central nervous system (CNS), with significant expression observed in various CNS regions including the amygdala, basal ganglia (caudate, putamen, and nucleus accumbens), substantia nigra, hippocampus, frontal cortex, and hypothalamus, particularly noteworthy is its exceptionally elevated expression in the spinal cord.
Interactions
GPR37 has been shown to interact with HSPA1A and Parkin (ligase). GPR37 is a receptor for prosaposin. It was previously thought to be a receptor for head activator, a neuropeptide found in the hydra, but early reports of head activator in mammals were never confirmed. To address challenges in confirming ligand-GPR37 interactions using recombinant GPR37 expressed in HEK293 cells, recent research has turned to primary cell cultures, leading to successful ligand identification. These investigations have unveiled the involvement of osteocalcin with GPR37 to regulate processes such as oligodendrocyte differentiation, myelination, myelin production, and remyelination following demyelinating injuries. Furthermore, osteocalcin treatment has demonstrated protective effects against Lipopolysaccharide-induced inflammation, which are absent in GPR37-deficient mice.
GPR37 signaling has been shown to modulate the migration of olfactory ensheathing cells (OECs) and gonadotropin-releasing hormone (GnRH) cells in mice.
References
Fu |
https://en.wikipedia.org/wiki/GPR39 | G-protein coupled receptor 39 is a protein that in humans is encoded by the GPR39 gene.
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Free%20fatty%20acid%20receptor%201 | Free fatty acid receptor 1 (FFAR1), also known as G-protein coupled receptor 40 (GPR40), is a rhodopsin-like G-protein coupled receptor that is coded (i.e., its synthesis is directed) by the FFAR1 gene. This gene is located on the short (i.e., "q") arm of chromosome 19 at position 13.12 (location notated as 19q13.12). G protein-coupled receptors (also termed GPRs or GPCRs) reside on their parent cells' surface membranes, bind any one of the specific set of ligands that they recognize, and thereby are activated to trigger certain responses in their parent cells. FFAR1 is a member of a small family of structurally and functionally related GPRs termed free fatty acid receptors (FFARs). This family includes at least three other FFARs viz., FFAR2 (also termed GPR43), FFAR3 (also termed GPR41), and FFAR4 (also termed GPR120). FFARs bind and thereby are activated by certain fatty acids.
Studies suggest that FFAR1 may be involved in the development of obesity, type 2 diabetes, and various emotional, behavioral, learning, and cognition defects such as Alzheimer's disease. FFAR1 may also be involved in the perception of pain, the tastes of and preferences for eating fatty and sweet foods, the pathological replacement of injured tissue with fibrosis and scarring, and the malignant behavior, i.e., proliferation, invasiveness, and metastasis, of some types of cancer cells.
Various fatty acids, including in particular two omega-3 fatty acids, docosahexaenoic and eicosapentaenoic acids, h |
https://en.wikipedia.org/wiki/Free%20fatty%20acid%20receptor%203 | Free fatty acid receptor 3 (FFA3) is a G-protein coupled receptor that in humans is encoded by the FFAR3 gene. It is a member of the free fatty acid receptors group of receptors.
Animal studies
Knockout mouse studies have implicated FFAR3 in diabetes, colitis, hypertension and asthma. However, discrepancies between the pathways activated by FFAR3 agonists in human cells and the equivalent murine counterparts have been observed.
Heteromerization
FFAR3 may interact with FFAR2 to form a FFAR2-FFAR3 receptor heteromer with signalling that is distinct from the parent homomers.
See also
Free fatty acid receptor
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR42 | Putative G-protein coupled receptor 42 is a protein that in humans is encoded by the GPR42P gene.
See also
Free fatty acid receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Free%20fatty%20acid%20receptor%202 | Free fatty acid receptor 2 (FFAR2), also termed G-protein coupled receptor 43 (GPR43), is a rhodopsin-like G-protein coupled receptor (also termed GPR or GPCR). It is coded (i.e., its synthesis is directed) by the FFAR2 gene. (FFAR2 and Ffar2 are used respectively to designate the human and animal genes for FFAR2.) In humans, the FFAR2 gene is located on the long (i.e., "q") arm of chromosome 19 at position 13.12 (location notated as 19q13.12). Like other GPCRs, FFAR2s reside on the surface membrane of cells and when bond to one of their activating ligands regulate the function of their parent cells. FFAR2 is a member of a small family of structurally and functionally related GPRs termed free fatty acid receptors (FFARs). This family includes three other receptors which, like FFAR2, are activated by certain fatty acids: FFAR1 (also termed GPR40), FFAR3 (GPR41), and FFAR4 (GPR120). FFAR2 and FFAR3 are activated by short-chain fatty acids whereas FFAR1 and FFAR4 are activated by long-chain fatty acids.
Short-chain fatty acids (i.e., SCFAs) are made by intestinal bacteria (intestinal and intestine are used here to mean the small intestine plus the large intestine's longest portion, the colon). These SCFAs are excreted from the bacteria, enter the hosts tissues, and stimulate cells in these tissues. This stimulation regulates many normal body functions but may result in the inhibition or promotion of various diseases and disorders. The types of bacteria in the intestines can be |
https://en.wikipedia.org/wiki/Piapot%2C%20Saskatchewan | Piapot () is a hamlet within the Rural Municipality of Piapot No. 110, Saskatchewan, Canada. Listed as a designated place by Statistics Canada, the hamlet had a population of 50 in the Canada 2016 Census.
Once a thriving community, it has seen a steady decline since the 1950s and in the present day it resembles a ghost town. The hotel and saloon closed in 2006 but reopened in May 2008, embracing western heritage and culture. The Piapot Saloon and Guesthouse offers an escape from everyday life in the spirit of the original settlers as well as a gift shop and old western saloon. The only other business that is open to the public is the post office.
Demographics
In the 2021 Census of Population conducted by Statistics Canada, Piapot had a population of 40 living in 22 of its 29 total private dwellings, a change of from its 2016 population of 50. With a land area of , it had a population density of in 2021.
See also
List of communities in Saskatchewan
List of hamlets in Saskatchewan
List of place names in Canada of Indigenous origin
Piapot
References
Piapot No. 110, Saskatchewan
Former villages in Saskatchewan
Designated places in Saskatchewan
Hamlets in Saskatchewan
Division No. 4, Saskatchewan |
https://en.wikipedia.org/wiki/Hypocretin%20%28orexin%29%20receptor%201 | Orexin receptor type 1 (Ox1R or OX1), also known as hypocretin receptor type 1 (HcrtR1), is a protein that in humans is encoded by the HCRTR1 gene.
Function
The orexin 1 receptor (OX1), is a G-protein coupled receptor that is heavily expressed in projections from the lateral hypothalamus and is involved in the regulation of feeding behaviour. OX1 selectively binds the orexin-A neuropeptide. It shares 64% identity with OX2.
Ligands
Agonists
Orexin-A
Antagonists
RTIOX-276 - Selective OX1 antagonist
ACT-335827 - Selective OX1 antagonist
Almorexant - Dual OX1 and OX2 antagonist
Lemborexant - Dual OX1 and OX2 antagonist
Nemorexant - Dual OX1 and OX2 antagonist
SB-334,867 - Selective OX1 antagonist
SB-408,124 - Selective OX1 antagonist
SB-649,868 - Dual OX1 and OX2 antagonist
Suvorexant - Dual OX1 and OX2 antagonist
See also
Orexin receptor
References
External links
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Hypocretin%20%28orexin%29%20receptor%202 | Orexin receptor type 2 (Ox2R or OX2), also known as hypocretin receptor type 2 (HcrtR2), is a protein that in humans is encoded by the HCRTR2 gene.
Structure
The structure of the receptor has been solved to 2.5 Å resolution as a fusion protein bound to suvorexant using lipid-mediated crystallization.
Function
OX2 is a G-protein coupled receptor expressed exclusively in the brain. It has 64% identity with OX1. OX2 binds both orexin A and orexin B neuropeptides. OX2 is involved in the central feedback mechanism that regulates feeding behaviour. Mice with enhanced OX2 signaling are resistant to high-fat diet-induced obesity.
This receptor is activated by Hipocretin, which is a wake-promoting hypothalamic neuropeptide that acts as a critical regulator of sleep in animals as Zebrafish or Mammals. This protein has mutations in Astyanax mexicanus that reduces the sleep needs of the cavefish.
Ligands
Agonists
Danavorexton (TAK-925) – selective OX2 receptor agonist
Firazorexton – selective OX2 receptor agonist
Orexins – dual OX1 and OX2 receptor agonists
Orexin-A – approximately equipotent at the OX1 and OX2 receptors
Orexin-B – approximately 5- to 10-fold selectivity for the OX2 receptor over the OX1 receptor
SB-668875 – selective OX2 receptor agonist
Suntinorexton – selective OX2 receptor agonist
TAK-861 – selective OX2 receptor agonist
TAK-994 – selective OX2 receptor agonist
Antagonists
Almorexant - Dual OX1 and OX2 antagonist
Daridorexant (nemorexant) - |
https://en.wikipedia.org/wiki/5-HT1E%20receptor | {{DISPLAYTITLE:5-HT1E receptor}}
5-hydroxytryptamine (serotonin) 1E receptor (5-HT1E) is a highly expressed human G-protein coupled receptor that belongs to the 5-HT1 receptor family (Gi-coupled serotonin receptor). The human gene is denoted as HTR1E.
Function
The function of the 5-HT1E receptor is unknown due to the lack of selective pharmacological tools, specific antibodies, and permissive animal models. The 5-HT1E receptor gene lacks polymorphisms amongst humans (few mutations), indicating a high degree of evolutionary conservation of genetic sequence, which suggests that the 5-HT1E receptor has an important physiological role in humans. It is hypothesized that the 5-HT1E receptor is involved in the regulation of memory in humans due to the high abundance of receptors in the frontal cortex, hippocampus, and olfactory bulb, all of which are regions of the brain integral to memory regulation.
This receptor is unique among the serotonin receptors in that it is not known to be expressed by rats or mouse species, all of which lack the gene encoding the 5-HT1E receptor. However the genomes of the pig, rhesus monkey, and several lagomorphs (including rabbit) as well as the guinea pig each encode a homologous 5-HT1E receptor gene. The guinea pig is the most likely candidate for future study of 5-HT1E receptor function in vivo. The expression of 5-HT1E receptors in the guinea pig brain has been pharmacologically confirmed; 5-HT1E receptor expression patterns of the human and |
https://en.wikipedia.org/wiki/5-HT1F%20receptor | {{DISPLAYTITLE:5-HT1F receptor}}
5-hydroxytryptamine (serotonin) receptor 1F, also known as HTR1F is a 5-HT1 receptor protein and also denotes the human gene encoding it.
Agonists
5-n-Butyryloxy-DMT: >60-fold selectivity versus 5-HT1E receptor
BRL-54443 - mixed 5-HT1E/1F agonist
Eletriptan - mixed 5-HT1B/1D/1E/1F/2B/7 agonist
LY-334,370 - as well as related benzamides
LY-344,864 (N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamide)
Naratriptan - mixed 5-HT1B/1D/1F agonist
Lasmiditan - selective 5-HT1F agonist, a first-in-class ditan molecule
Antagonists
MLS000756415
See also
5-HT1 receptor
5-HT receptor
References
Further reading
External links
Serotonin receptors |
https://en.wikipedia.org/wiki/5-HT2B%20receptor | {{DISPLAYTITLE:5-HT2B receptor}}
5-Hydroxytryptamine receptor 2B (5-HT2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the HTR2B gene. 5-HT2B is a member of the 5-HT2 receptor family that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT).
Tissue distribution and function
First discovered in the stomach of rats, 5-HT2B was challenging to characterize initially because of its structural similarity to the other 5-HT2 receptors, particularly 5-HT2C. The 5-HT2 receptors (of which the 5-HT2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of serotonin. Cardiovascular effects include contraction of blood vessels and shape changes in platelets; central nervous system (CNS) effects include neuronal sensitization to tactile stimuli and mediation of some of the effects of hallucinogenic substituted amphetamines. The 5-HT2B receptor is expressed in several areas of the CNS, including the dorsal hypothalamus, frontal cortex, medial amygdala, and meninges. However, its most important role is in the peripheral nervous system (PNS) where it maintains the viability and efficiency of the cardiac valve leaflets.
The 5-HT2B receptor subtype is involved in:
CNS: inhibition of serotonin and dopamine uptake, behavioral effects
Vascular: pulmonary vasoconstriction
Cardiac: The 5-HT2B receptor regulates cardiac structure and functions, as demonstrated by the abnormal cardiac development observed in 5-HT2B r |
https://en.wikipedia.org/wiki/5-HT5A%20receptor | {{DISPLAYTITLE:5-HT5A receptor}}
5-Hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein that in humans is encoded by the HTR5A gene. Agonists and antagonists for 5-HT receptors, as well as serotonin uptake inhibitors, present promnesic (memory-promoting) and/or anti-amnesic effects under different conditions, and 5-HT receptors are also associated with neural changes.
Function
The gene described in this record is a member of 5-hydroxytryptamine receptor family and encodes a multi-pass membrane protein that functions as a receptor for 5-hydroxytryptamine and couples to G proteins, negatively influencing cAMP levels via Gi and Go. This protein has been shown to function in part through the regulation of intracellular Ca2+ mobilization. The 5-HT5A receptor has been shown to be functional in a native expression system.
Rodents have been shown to possess two functional 5-HT5 receptor subtypes, 5-HT5A and 5-HT5B, however while humans possess a gene coding for the 5-HT5B subtype, its coding sequence is interrupted by stop codons, making the gene non-functional, and so only the 5-HT5A subtype is expressed in human brain.
It also appears to serve as a presynaptic serotonin autoreceptor.
Clinical significance
The neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) has been implicated in a wide range of psychiatric conditions and also has vasoconstrictive and vasodilatory effects.
Selective ligands
Few highly selective ligands are commercially avai |
https://en.wikipedia.org/wiki/5-HT6%20receptor | {{DISPLAYTITLE:5-HT6 receptor}}
The 5HT6 receptor is a subtype of 5HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5HT). It is a G protein-coupled receptor (GPCR) that is coupled to Gs and mediates excitatory neurotransmission. HTR6 denotes the human gene encoding for the receptor.
Distribution
The 5HT6 receptor is expressed almost exclusively in the brain. It is distributed in various areas including, but not limited to, the olfactory tubercle, cerebral cortex (frontal and entorhinal regions), nucleus accumbens, striatum, caudate nucleus, hippocampus, and the molecular layer of the cerebellum. Based on its abundance in extrapyramidal, limbic, and cortical regions it can be suggested that the 5HT6 receptor plays a role in functions like motor control, emotionality, cognition, and memory.
Function
Blockade of central 5HT6 receptors has been shown to increase glutamatergic and cholinergic neurotransmission in various brain areas, whereas activation enhances GABAergic signaling in a widespread manner. Antagonism of 5HT6 receptors also facilitates dopamine and norepinephrine release in the frontal cortex, while stimulation has the opposite effect.
As a drug target for antagonists
Despite the 5HT6 receptor having a functionally excitatory action, it is largely co-localized with GABAergic neurons and therefore produces an overall inhibition of brain activity. In parallel with this, 5HT6 antagonists are hypothesized to improve cognition, l |
https://en.wikipedia.org/wiki/Melanocortin%203%20receptor | Melanocortin 3 receptor (MC3R) is a protein that in humans is encoded by the gene.
Function
This gene encodes MC3R, a G-protein coupled receptor (GPCR) for melanocyte-stimulating hormone (MSH) and adrenocorticotropic hormone (ACTH) that is expressed in the brain. This gene maps to the same region as the locus for benign neonatal epilepsy. Mice deficient for this gene have increased fat mass, reduced lean mass and decreased food intake, all suggesting a role for the receptor in the regulation of energy homeostasis. MC3R mutations has been linked to reduced growth rate during childhood and a delay in the age of puberty onset.
Research
Studies performed by the Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD), found that two specific polymorphisms in the MC3R gene may be associated with pediatric obesity and greater body mass because of greater energy intake. Children who were homozygous for C17A + G241A consumed approximately 38% more than those who did not contain aforementioned polymorphisms. The study concluded that these genetic variants did not affect energy expenditure.
Ligands
Ac-Val-Gln-(pI)DPhe-DTic-NH2, first MC3 selective agonist, 100x selectivity over MC4.
Ac-Val-Gln-DBip-DTic-NH2, 140x selectivity over MC4.
Pyrrolidine bis-cyclic guanidines, non-peptide small molecule MC3 agonists, good selectivity over MC4 but not over MC1 or MC5.
SHU-9119, mixed MC3/MC4 antagonist.
See also
Melanocortin receptor
References
Furth |
https://en.wikipedia.org/wiki/Melanocortin%205%20receptor | Melanocortin 5 receptor (MC5R) is a protein that in humans is encoded by the gene. It is located on the chromosome 18 in the human genome. When the MC5R was disrupted in transgenic mice, it induced disruption of their exocrine glands and resulted in decreased production of sebum.
Physiology
MC5R is necessary for normal sebum production. Stimulation of MC5R promotes fatty acid oxidation in skeletal muscle and lypolysis in adipocytes. MC5R is essential for erythrocyte differentiation. MC5R is involved in inflammation. MC5R helps maintain thermal homeostasis.
MC5R is expressed in the brain at different levels depending on physical activity.
Pheromones
MC5R is heavily expressed in the preputial gland in mice (a modified sebaceous gland involved in pheromone production). MC5R deficiency in male mice decreases aggressive behavior, promotes defensive behavior and encourages other male mice to attack MC5R-deficient males through pheromonal signals.
MRAP
Melanocortin 2 receptor accessory protein (MRAP) traps MC5R protein inside cells.
See also
Melanocortin receptor
References
Further reading
External links
G protein-coupled receptors
Human proteins |
https://en.wikipedia.org/wiki/Melatonin%20receptor%201A | Melatonin receptor type 1A is a protein that in humans is encoded by the MTNR1A gene.
Function
This gene encodes the MT1 protein, one of two high-affinity forms of a receptor for melatonin, the primary hormone secreted by the pineal gland. This receptor is a G protein-coupled, 7-transmembrane receptor that is responsible for melatonin effects on mammalian circadian rhythm and reproductive alterations affected by day length. The receptor is an integral membrane protein that is readily detectable and localized to two specific regions of the brain. The hypothalamic suprachiasmatic nucleus appears to be involved in circadian rhythm while the hypophysial pars tuberalis may be responsible for the reproductive effects of melatonin.
Ligands
Melatonin – full agonist
Afobazole – agonist
Agomelatine – agonist
See also
Melatonin receptor
Discovery and development of melatonin receptor agonists
References
Further reading
G protein-coupled receptors
Human proteins
1A |
https://en.wikipedia.org/wiki/Neuropeptide%20Y%20receptor%20Y1 | Neuropeptide Y receptor type 1 is a protein that in humans is encoded by the NPY1R gene.
Selective ligands
Agonists
Neuropeptide Y (endogenous agonist, non subtype selective)
Peptide YY
Antagonists
Peptide
BVD-10 (selective NPY1 antagonist, CAS# 262418-00-8)
GR-231,118 (mixed NPY1 antagonist / NPY4 agonist, CAS# 158859-98-4)
Non-peptide
BIBO-3304 (CAS# 191868-14-1)
BIBP-3226 (CAS# 159013-54-4)
PD-160,170 (CAS# 181468-88-2)
Available Structures
5ZBH (Neuropeptide Y1 bound to antagonist BMS-193835)
5ZBQ (Neuropeptide Y1 bound to antagonist UR-MK299)
See also
Neuropeptide Y receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Neuropeptide%20Y%20receptor%20Y2 | Neuropeptide Y receptor type 2 (Y2R) is a member of the neuropeptide Y receptor family of G-protein coupled receptors, that in humans is encoded by the NPY2R gene.
Selective ligands
Agonists
Neuropeptide Y (endogenous agonist, non subtype selective)
Neuropeptide Y fragment 13-36 (NPY2 selective agonist)
Peptide YY
Peptide YY 3-36 fragment
Antagonists
BIIE-0246 (CAS# 246146-55-4)
JNJ 5207787 (CAS# 683746-68-1)
SF 11 (CAS# 443292-81-7)
See also
Neuropeptide Y receptor
References
External links
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Neuropeptide%20Y%20receptor%20Y6 | Putative neuropeptide Y receptor type 6 is a protein that in humans is encoded by the NPY6R gene.
References
Further reading |
https://en.wikipedia.org/wiki/Neuropeptide%20Y%20receptor%20Y5 | Neuropeptide Y receptor type 5 is a protein that in humans is encoded by the NPY5R gene.
Selective ligands
Agonists
Neuropeptide Y (endogenous agonist, non subtype selective)
BWX-46 (selective NPY5 agonist, CAS# 172997-92-1)
Peptide YY
Antagonists
CGP-71683 (CAS# 192322-50-2)
FMS-586
L-152,804 (CAS# 6508-43-6)
Lu AA-33810
MK-0557
NTNCB (CAS# 486453-65-0)
Velneperit (S-2367)
See also
Neuropeptide Y receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR143 | G-protein coupled receptor 143, also known as Ocular albinism type 1 (OA1) in humans, is a conserved integral membrane protein with seven transmembrane domains and similarities with G protein-coupled receptors (GPCRs) that is expressed in the eye and epidermal melanocytes. This protein encoded by the GPR143 gene, whose variants can lead to Ocular albinism type 1.
The GPR143 gene is regulated by the Microphthalmia-associated transcription factor.
L-DOPA is an endogenous ligand for OA1.
Interactions
GPR143 has been shown to interact with GNAI1.
References
Further reading
External links
GeneReviews/NCBI/NIH/UW entry on Ocular Albinism, X-Linked
G protein-coupled receptors |
https://en.wikipedia.org/wiki/P2RY6 | P2Y purinoceptor 6 is a protein that in humans is encoded by the P2RY6 gene.
Function
The product of this gene, P2Y6, belongs to the family of G-protein coupled receptors. This family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. This receptor is responsive to UDP, partially responsive to UTP and ADP, and not responsive to ATP. Four transcript variants encoding the same isoform have been identified for this gene.
See also
P2Y receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/P2RY11 | P2Y purinoceptor 11 is a protein that in humans is encoded by the P2RY11 gene.
The product of this gene, P2Y11, belongs to the family of G-protein coupled receptors. This family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. This receptor is coupled to the stimulation of the phosphoinositide and adenylyl cyclase pathways and behaves as a selective purinoceptor. Naturally occurring read-through transcripts, resulting from intergenic splicing between this gene and an immediately upstream gene (PPAN, encoding peter pan homolog), have been found. The PPAN-P2RY11 read-through mRNA is ubiquitously expressed and encodes a fusion protein that shares identity with each individual gene product.
See also
P2Y receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Parathyroid%20hormone%202%20receptor | Parathyroid hormone 2 receptor is a protein that in humans is encoded by the PTH2R gene.
Function
The protein encoded by this gene is a member of the G protein-coupled receptor family 2. This protein is a receptor for parathyroid hormone (PTH). This receptor is more selective in ligand recognition and has a more specific tissue distribution compared to parathyroid hormone 1 receptor (PTH1R). It is activated by PTH but not by parathyroid hormone-like hormone (PTHLH) and is particularly abundant in the brain and pancreas.
The molecular interaction of the PTH2 receptor with the peptide TIP39 has been characterized in full 3D molecular detail, identifying among other residues Tyr-318 in transmembrane helix 5 as a key residue for high affinity binding.
See also
Parathyroid hormone receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Somatostatin%20receptor%201 | Somatostatin receptor type 1 is a protein that in humans is encoded by the SSTR1 gene.
Function
Somatostatin acts at many sites to inhibit the release of many hormones and other secretory proteins. The biological effects of somatostatin are probably mediated by a family of G protein-coupled receptors that are expressed in a tissue-specific manner. The encoded protein is a member of the superfamily of somatostatin receptors having seven transmembrane segments, and is expressed in highest levels in jejunum and stomach.
See also
Somatostatin receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Somatostatin%20receptor%203 | Shekel Somatostatin receptor type 3 is a protein that in humans is encoded by the SSTR3 gene.
Function
Somatostatin acts at many sites to inhibit the release of many hormones and other secretory proteins. The biological effects of somatostatin are probably mediated by a family of G protein-coupled receptors that are expressed in a tissue-specific manner. SSTR3 is a member of the superfamily of receptors having seven transmembrane segments and is expressed in highest levels in brain and pancreatic islets. SSTR3 is functionally coupled to adenylyl cyclase.
See also
Somatostatin receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Somatostatin%20receptor%204 | Somatostatin receptor type 4 is a protein that in humans is encoded by the SSTR4 gene.
Function
Somatostatin acts at many sites to inhibit the release of many hormones and other secretory proteins. The biologic effects of somatostatin are probably mediated by a family of G protein-coupled receptors that are expressed in a tissue-specific manner. SSTR4 is a member of the superfamily of receptors having seven transmembrane segments and is expressed in highest levels in fetal and adult brain and lung.
See also
Somatostatin receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Tachykinin%20receptor%202 | Substance-K receptor is a protein that in humans is encoded by the TACR2 gene.
Function
This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neuropeptide substance K, also referred to as neurokinin A.
Selective Ligands
Several selective ligands for NK2 are now available, and although most of the compounds developed so far are peptides, one small-molecule antagonist Saredutant is currently in clinical trials as an anxiolytic and antidepressant.
Agonists
GR-64349 - potent and selective agonist, EC50 3.7nM, 7-amino acid polypeptide chain. CAS# 137593-52-3
Antagonists
Ibodutant - failed its Phase 3 trial for IBS treatment in 2015, and abandoned by Menarini
Saredutant - mixed but mostly negative Phase 3 trial results in 2009, and abandoned by Sanofi-Aventis
GR-159897
MEN-10376 - potent and selective antagonist, 7-amino acid polypeptide chain. CAS# 135306-85-3
See also
Tachykinin receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Tachykinin%20receptor%203 | Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.
Function
This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neurokinin 3, also referred to as neurokinin B.
Selective ligands
A number of selective ligands are available for NK3. NK3 receptor antagonists are being investigated as treatments for various indications.
Agonists
Neurokinin B – endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK3
Senktide – 7-amino acid polypeptide, NK3 selective, CAS# 106128-89-6
Antagonists
Elinzanetant (BAY-3427080 GSK-1144814, NT-814)
Fezolinetant (ESN-364)
Osanetant (SR-142,801)
Pavinetant (MLE-4901, AZD-4901, AZD-2624)
Talnetant (SB-223,412)
SB-222,200 – potent and selective antagonist, Ki = 4.4 nM, 3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide, CAS# 174635-69-9
SB-218,795 – more selective than SB-222,200, Ki = 13 nM, (R)-[(2-Phenyl-4-quinolinylcarbonyl)amino]-methyl ester benzeneacetic acid, CAS# 174635-53-1
See also
Tachykinin receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/VIPR2 | Vasoactive intestinal peptide receptor 2 also known as VPAC2, is a G-protein coupled receptor that in humans is encoded by the VIPR2 gene.
Tissue distribution
VIPR2 is expressed in the uterus, prostate, smooth muscle of the gastrointestinal tract, seminal vesicles and skin, blood vessels and thymus. VIPR2 is also expressed in the cerebellum.
Function
Vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase activating polypeptide (PACAP) are homologous peptides that function as neurotransmitters and neuroendocrine hormones. While the receptors for VIP (VIRP 1 and 2) and PACAP (ADCYAP1R1) share homology, they differ in their substrate specificities and expression patterns. VIPR2 transduction results in upregulation of adenylate cyclase activity. Furthermore, VIPR2 mediates the anti-inflammatory effects of VIP.
Research using VPAC2 knockout mice implicate it in the function of the circadian clock, growth, basal energy expenditure and male reproduction.
VIPR2 and/or PAC1 receptor activation is involved in cutaneous active vasodilation in humans.
Splice variants may modify the immunoregulatory contributions of the VIP-VIPR2 axis.
VIPR2 may contribute to autoregulation and/or coupling within the suprachiasmatic nucleus (SCN) core and to control of the SCN shell.
Clinical significance
VIPR2 may play a role in schizophrenia.
The abnormal expression of VIPR2 messenger RNA in gallbladder tissue may play a role in the formation of gall stones and polyps.
See also
|
https://en.wikipedia.org/wiki/Frizzled-5 | Frizzled-5 (Fz-5) is a protein that in humans is encoded by the FZD5 gene.
Members of the 'frizzled' gene family encode 7-transmembrane domain proteins that are receptors for Wnt signaling proteins. Fz-5 is believed to be the receptor for the Wnt5A ligand.
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Frizzled-3 | Frizzled-3 (Fz-3) is a protein that in humans is encoded by the FZD3 gene.
Function
This gene is a member of the frizzled gene family. Members of this family encode seven-transmembrane domain proteins that are receptors for the Wingless type MMTV integration site family of signaling proteins. Most frizzled receptors are coupled to the beta-catenin canonical signaling pathway. It may play a role in mammalian hair follicle development.
The function of this gene is largely derived from mouse studies. Fzd3 in the mouse functions through planar cell polarity signaling instead of the canonical Wnt/beta-catenin pathway. Fzd3 controls axon growth and guidance in the mouse nervous system, and migration of neural crest cells.
See also
Frizzled
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR68 | Ovarian cancer G-protein coupled receptor 1 is a protein that in humans is encoded by the GPR68 gene.
See also
Proton-sensing G protein-coupled receptors
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Frizzled-1 | Frizzled-1 (Fz-1) is a protein that in humans is encoded by the FZD1 gene.
Function
Members of the 'frizzled' gene family encode 7-transmembrane domain proteins that are receptors for Wnt signaling proteins. The FZD1 protein contains a signal peptide, a cysteine-rich domain in the N-terminal extracellular region, 7 transmembrane domains, and a C-terminal PDZ domain-binding motif. The FZD1 transcript is expressed in various tissues.
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Frizzled-6 | Frizzled-6 (Fz-6) is a protein that in humans is encoded by the FZD6 gene.
Members of the 'frizzled' gene family encode 7-transmembrane domain proteins that are receptors for WNT signaling proteins. The FZD6 protein contains a signal peptide, a cysteine-rich domain in the N-terminal extracellular region, and 7 transmembrane domains. However, unlike many other FZD family members, FDZ6 does not contain a C-terminal PDZ domain-binding motif. Fz-6 is believed to be the receptor for the WNT4 ligand.
Interactions
Fz-6 has been shown to interact with secreted frizzled-related protein 1.
Model organisms
Model organisms have been used in the study of FXYD3 function. In 2004, researchers at the Howard Hughes Medical Institute showed that FZD6 controls hair patterning in mice, and its human homologue is understood to play a part in the formation of hair whorls and cowlicks. A conditional knockout mouse line called Fxyd3tm1a(KOMP)Wtsi was generated at the Wellcome Trust Sanger Institute. Male and female animals underwent a standardized phenotypic screen to determine the effects of deletion. Additional screens performed: - In-depth immunological phenotyping
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Frizzled-7 | Frizzled-7 (Fd-7) is a protein that in humans is encoded by the FZD7 gene.
Members of the 'frizzled' gene family encode 7-transmembrane domain proteins that are receptors for Wnt signaling proteins. The FZD7 protein contains an N-terminal signal sequence, 10 cysteine residues typical of the cysteine-rich extracellular domain of Fz family members, 7 putative transmembrane domains, and an intracellular C-terminal tail with a PDZ domain-binding motif. FZD7 gene expression may downregulate APC function and enhance beta-catenin-mediated signals in poorly differentiated human esophageal carcinomas.
Interactions
Fz-7 has been shown to interact with DLG4.
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Frizzled-8 | Frizzled-8 (Fz-8) is a protein that in humans is encoded by the FZD8 gene.
Function
This intronless gene is a member of the frizzled gene family. Members of this family encode seven-transmembrane domain proteins that are receptors for the Wingless type MMTV integration site family of signaling proteins. Most frizzled receptors are coupled to the beta-catenin canonical signaling pathway. This gene is highly expressed in two human cancer cell lines, indicating that it may play a role in several types of cancer. The crystal structure of the extracellular cysteine-rich domain of a similar mouse protein has been determined.
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Frizzled-9 | Frizzled-9 (Fz-9) is a protein that in humans is encoded by the FZD9 gene. Fz-9 has also been designated as CD349 (cluster of differentiation 349).
Function
Members of the 'frizzled' gene family encode 7-transmembrane domain proteins that are receptors for Wnt signaling proteins. The FZD9 gene is located within the Williams syndrome common deletion region of chromosome 7, and heterozygous deletion of the FZD9 gene may contribute to the Williams syndrome phenotype. FZD9 is expressed predominantly in brain, testis, eye, skeletal muscle, and kidney.
References
Further reading
External links
Clusters of differentiation
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR65 | Psychosine receptor is a G protein-coupled receptor (GPCR) protein that in humans is encoded by the GPR65 gene. GPR65 is also referred to as TDAG8.
Species, tissue, and subcellular distribution
GPR65 (TDAG8) is primarily expressed in lymphoid tissues (spleen, lymph nodes, thymus, and leukocytes), and as a GPCR, the protein is localized to the plasma membrane.
Function
Ligand binding
In 2001, GPR65 was reported to be a specific receptor for psychosine (d-galactosyl-β-1,1′ sphingosine) as well as several other related glycosphingolipids. However, the specific binding of psychosine to GPR65 has been contested as the reported ligand binding did not satisfy the appropriate pharmacological criteria.
More recently, 3-[(2,4-dichlorophenyl)methylsulfanyl]-1,6-dimethylpyridazino[4,5-e][1,3,4]thiadiazin-5-one (referred to as BTB09089) was found to be a specific agonist for GPR65. Furthermore, [(S)-phenyl(pyridin-4-yl)methyl] 4-methyl-2-pyrimidin-2-yl-1,3-thiazole-5-carboxylate (referred to as ZINC62678696) was found to act as a BTB09089 negative allosteric modulator.
pH sensing
GPR65 senses extracellular pH. Levels of cyclic adenosine monophosphate (cAMP), a secondary messenger associated with activation of GPCRs in the cAMP-dependent pathway, were found to be elevated in neutral to acidic extracellular pH (pH 7.0-6.5) in cells expressing GPR65. In cells with mutated GPR65, this pH-sensing effect was reduced or eliminated. In the presence of psychosine, however, the levels of c |
https://en.wikipedia.org/wiki/Galanin%20receptor%203 | Galanin receptor 3 (GAL3) is a G-protein coupled receptor encoded by the GALR3 gene.
Function
The neuropeptide galanin modulates a variety of physiologic processes including cognition/memory, sensory/pain processing, hormone secretion, and feeding behavior. The human galanin receptors are G protein-coupled receptors that functionally couple to their intracellular effector through distinct signaling pathways. GALR3 is found in many tissues and may be expressed as 1.4-, 2.4-, and 5-kb transcripts
See also
Galanin receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/S1PR4 | Sphingosine-1-phosphate receptor 4 also known as S1PR4 is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P). Hence this receptor is also known as S1P4.
Function
This gene is a member of the endothelial differentiation, G-protein-coupled (EDG) receptor gene family. EDG receptors bind lysophospholipids or lysosphingolipids as ligands, and are involved in cell signalling in many different cell types. This EDG receptor gene is intronless and is specifically expressed in the lymphoid tissue.
See also
Lysophospholipid receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Galanin%20receptor%202 | Galanin receptor 2, (GAL2) is a G-protein coupled receptor encoded by the GALR2 gene.
Function
Galanin is an important neuromodulator present in the brain, gastrointestinal system, and hypothalamopituitary axis. It is a 30-amino acid non-C-terminally amidated peptide that potently stimulates growth hormone secretion, inhibits cardiac vagal slowing of heart rate, abolishes sinus arrhythmia, and inhibits postprandial gastrointestinal motility. The actions of galanin are mediated through interaction with specific membrane receptors that are members of the 7-transmembrane family of G protein-coupled receptors. GALR2 interacts with the N-terminal residues of the galanin peptide. The primary signaling mechanism for GALR2 is through the phospholipase C/protein kinase C pathway (via Gq), in contrast to GALR1, which communicates its intracellular signal by inhibition of adenylyl cyclase through Gi. However, it has been demonstrated that GALR2 couples efficiently to both the Gq and Gi proteins to simultaneously activate 2 independent signal transduction pathways.
See also
Galanin receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Hydroxycarboxylic%20acid%20receptor%203 | Hydroxycarboxylic acid receptor 3 (HCA3), also known as niacin receptor 2 (NIACR2) and GPR109B, is a protein which in humans is encoded by the HCAR3 gene. HCA3, like the other hydroxycarboxylic acid receptors HCA1 and HCA2, is a G protein-coupled receptor (GPCR). The primary endogenous agonists of HCA3 are 3-hydroxyoctanoic acid and kynurenic acid. HCA3 is also a low-affinity biomolecular target for niacin (aka nicotinic acid).
References
External links
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/F2RL3 | Protease-activated receptor 4 (PAR-4), also known as coagulation factor II (thrombin) receptor-like 3, is a protein that in humans is encoded by the F2RL3 gene.
Function
Coagulation factor II (thrombin) receptor-like 3 (F2RL3) is a member of the large family of 7-transmembrane-region receptors that couple to guanosine-nucleotide-binding proteins. F2RL3 is also a member of the protease-activated receptor family. F2RL3 is activated by proteolytic cleavage of its extracellular amino terminus. The new amino terminus functions as a tethered ligand and activates the receptor. F2RL3 is activated by thrombin and trypsin.
See also
Protease-activated receptor
References
Further reading
Receptors
G protein-coupled receptors |
https://en.wikipedia.org/wiki/LPAR2 | Lysophosphatidic acid receptor 2 also known as LPA2 is a protein that in humans is encoded by the LPAR2 gene. LPA2 is a G protein-coupled receptor that binds the lipid signaling molecule lysophosphatidic acid (LPA).
Function
This gene encodes a member of family I of the G protein-coupled receptors, as well as the EDG family of proteins. This protein functions as a lysophosphatidic acid (LPA) receptor and contributes to Ca2+ mobilization, a critical cellular response to LPA in cells, through association with Gi and Gq proteins.
Interactions
LPAR2 has been shown to interact with TRIP6.
See also
Lysophospholipid receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR37L1 | Endothelin B receptor-like protein 2 is a protein that in humans is encoded by the GPR37L1 gene.
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/TAAR2 | Trace amine-associated receptor 2 (TAAR2), formerly known as G protein-coupled receptor 58 (GPR58), is a protein that in humans is encoded by the TAAR2 gene. TAAR2 is coexpressed with Gα proteins; however, its signal transduction mechanisms have not been determined.
Tissue distribution
Human TAAR2 (hTAAR2) is expressed in the cerebellum, olfactory sensory neurons in the olfactory epithelium, and leukocytes (i.e., white blood cells), among other tissues. hTAAR1 and hTAAR2 are both required for white blood cell activation by trace amines in granulocytes.
Using brain histochemistry staining of mice with LacZ insertion into TAAR2 gene histochemical reaction was found in the glomerular layer of the olfactory bulb, but intensive staining was found in the deeper layer as well. The histochemical reaction was observed in the fibers of the olfactory nerve, in the glomeruli of the glomerular layer, several short axon (SA) cells (outer plexiform layer or granular layer) and neuronal projections that were visualized throughout the depth of the olfactory bulb. Furthermore, LacZ staining was observed in the limbic areas of the brain receiving olfactory input, i.e., piriform cortex molecular area, hippocampus (CA1 field, pyramidal layer), hypothalamic lateral zone (zone incerta) and lateral habenula. In addition, a histochemical reaction was found in the midbrain raphe nuclei and primary somatosensory area of the cortex (layer 5). Real-time quantitative PCR with reverse transcription co |
https://en.wikipedia.org/wiki/TAAR3 | Putative trace amine-associated receptor 3 (TAAR3) is a human pseudogene with the gene symbol TAAR3P. In other species such as mice, TAAR3 is a functional protein-coding gene that encodes a trace amine-associated receptor protein.
Isobutylamine is a known ligand of TAAR3 in mice associated with sexual behaviour in male mice.
Isopentylamine was identified as a ligand for murine TAAR3 eliciting aversive behavior.
See also
Trace amine-associated receptor
References
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR55 | G protein-coupled receptor 55 also known as GPR55 is a G protein-coupled receptor that in humans is encoded by the GPR55 gene.
GPR55, along with GPR119 and GPR18, have been implicated as novel cannabinoid receptors.
History
GPR55 was identified and cloned for the first time in 1999. Later it was identified by an in silico screen as a putative cannabinoid receptor because of a similar amino acid sequence in the binding region. Research groups from Glaxo Smith Kline and Astra Zeneca characterized the receptor extensively because it was hoped to be responsible for the blood pressure lowering properties of cannabinoids. GPR55 is indeed activated by endogenous and exogenous cannabinoids such as plant and synthetic cannabinoids but GPR-55 knockout mice generated by a research group from Glaxo Smith Kline showed no altered blood pressure regulation after administration of the cannabidiol-derivative abnormal cannabidiol.
Signal cascade
GPR55 is coupled to the G-protein G13 and activation of the receptor leads to stimulation of rhoA, cdc42 and rac1.
Pharmacology
GPR55 is activated by the plant cannabinoids Δ9-THC and the endocannabinoids anandamide, 2-AG and noladin ether in the low nanomolar range. Exocannabinoids such as the synthetic cannabinoid CP-55940 are also able to activate the receptor while the structurally unrelated cannabinoid mimic WIN 55,212-2 fails to activate the receptor. Recent research suggests that lysophosphatidylinositol and its 2-arachidonoyl derivati |
https://en.wikipedia.org/wiki/GPR52 | Probable G-protein coupled receptor 52 is a protein that in humans is encoded by the GPR52 gene.
Members of the G protein-coupled receptor (GPR) family play important roles in signal transduction from the external environment to the inside of the cell.[supplied by OMIM]
Cannabidiol, CBD, and O-1918 are Inverse agonist at GPR52
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/S1PR2 | Sphingosine-1-phosphate receptor 2, also known as S1PR2 or S1P2, is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P).
Function
This protein participates in sphingosine 1-phosphate-induced cell proliferation, survival, and transcriptional activation. It has also been shown to interact with Nogo-A (RTN4), an neurite outgrowth inhibitor. S1PR2 is expressed in neuronal and vascular cells and is crucial for the migration and growth of developing and injured neuronal and vascular system.
See also
Lysophospholipid receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GABBR2 | Gamma-aminobutyric acid (GABA) B receptor, 2 (GABAB2) is a G-protein coupled receptor subunit encoded by the GABBR2 gene in humans.
Function
B-type receptors for the neurotransmitter GABA (gamma-aminobutyric acid) inhibit neuronal activity through G protein-coupled second-messenger systems, which regulate the release of neurotransmitters and the activity of ion channels and adenylyl cyclase. See GABBR1 (MIM 603540) for additional background information on GABA-B receptors.[supplied by OMIM]
Interactions
GABBR2 has been shown to interact with GABBR1.
See also
GABAB receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/P2RY14 | P2Y purinoceptor 14 is a protein that in humans is encoded by the P2RY14 gene.
The product of this gene, P2Y14 belongs to the family of G-protein coupled receptors, which contains several receptor subtypes with different pharmacological selectivity for various adenosine and uridine nucleotides. This receptor is a P2Y purinergic receptor for UDP-glucose and other UDP-sugars coupled to G-proteins. It has been implicated in extending the known immune system functions of P2Y receptors by participating in the regulation of the stem cell compartment, and it may also play a role in neuroimmune function. Two transcript variants encoding the same protein have been identified for this gene.
See also
P2Y receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR64 | G protein-coupled receptor 64 also known as HE6 is a protein encoded by the ADGRG2 gene. GPR64 is a member of the adhesion GPCR family.
Adhesion GPCRs are characterized by an extended extracellular region often possessing N-terminal protein modules that is linked to a TM7 region via a domain known as the GPCR-Autoproteolysis INducing (GAIN) domain.
The adhesion GPCR, GPR64, is an orphan receptor characterized by a long N-terminus with that has been suggested to be highly glycosylated. GPR64's N-terminus has been reported to be cleaved at the GPS domain to allow for trafficking to the plasma membrane. After cleavage the N-terminus is believed to remain non-covalently associated with the 7TM. GPR64 expression has been mostly reported in the male reproductive organs, but more recently has been shown to be expressed in the parathyroid glands and central nervous system. GPR64 is mainly expressed in human and mouse epididymis as well as human prostate and parathyroid. GPR64, together with F-actin scaffold, locates at the nonciliated principal cells of the proximal male excurrent duct epithelia, where reabsorption of testicular fluid and concentration of sperm takes place.
Function
Targeting of Gpr64 in mice causes reduced fertility or infertility in males; but the reproductive capacity was unaffected in females. Unchanged hormone expression in knockout males indicates that the receptor functions immediately in the male genital tract. Lack of Gpr64 expression causes sperm stasi |
https://en.wikipedia.org/wiki/LPAR6 | Lysophosphatidic acid receptor 6, also known as LPA6, P2RY5 and GPR87, is a protein that in humans is encoded by the LPAR6 gene. LPA6 is a G protein-coupled receptor that binds the lipid signaling molecule lysophosphatidic acid (LPA).
The protein encoded by this gene belongs to the family of G-protein coupled receptors, that are preferentially activated by adenosine and uridine nucleotides. This gene aligns with an internal intron of the retinoblastoma susceptibility gene in the reverse orientation.
Role in hair growth/loss
In February 2008, researchers at the University of Bonn announced they have found the genetic basis of two distinct forms of inherited hair loss, opening a broad path to treatments for baldness. They found that mutations in the gene P2RY5 causes a rare, inherited form of hair loss called hypotrichosis simplex. It is the first receptor in humans known to play a role in hair growth. The fact that any receptor plays a specific role in hair growth was previously unknown to scientists, and with this new knowledge a focus on finding more of these genes may be able to lead to therapies for many different types of hair loss.
In 2013, it was found that mutations in LPAR6 give rise to the Cornish Rex cat breed, which has a form of ectodermal dysplasia characterised by short woolly hair which is susceptible to loss.
See also
Lysophospholipid receptor
P2Y receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/RRH | Peropsin, a visual pigment-like receptor, is a protein that in humans is encoded by the RRH gene. It belongs like other animal opsins to the G protein-coupled receptors. Even so, the first peropsins were already discovered in mice and humans in 1997, not much is known about them.
Photochemistry
Like most opsins, peropsins have in its seventh transmembrane domain a lysine corresponding to amino acid position 296 in cattle rhodopsin, which is important for retinal binding and light sensing.
In amphioxus, a cephalochordate, a peropsin binds in the dark-state all-trans-retinal instead of 11-cis-retinal, as it is in cattle rhodopsin. Therefore, peropsins have been suggested to be photoisomerases.
Tissue localization
In mice, a peropsin is localized to the apical microvilli of the retinal pigment epithelium (RPE). There, it regulates storage or the movement of vitamin A from the retina to the RPE. A peropsin is also expressed in keratinocytes of the human skin. In keratinocyte cell culture, it reacts to UV light if retinal is supplied. In chicken, a peropsin is expressed with an RGR-opsin in the pineal gland and the retina.
Gene localization and structure
The human peropsin gene lies on chromosome 4 band 4q25 and has six introns like RGR-opsins. However only two of these introns are inserted at the same place, which still indicates that peropsins and RGR-opsins are more closely related to each other than to the ciliary and rhabdomeric opsins. This shared gene structure is al |
https://en.wikipedia.org/wiki/CCR9 | C-C chemokine receptor type 9 is a protein that in humans is encoded by the CCR9 gene. This gene is mapped to the chemokine receptor gene cluster region. Two alternatively spliced transcript variants have been described.
CCR9 has also recently been designated CDw199 (cluster of differentiation w199).
The protein encoded by this gene is a member of the beta chemokine receptor family. CCR9 is a seven transmembrane protein similar to G protein-coupled receptors.
Function
Chemokines and their receptors, such as CCR9 and its binding agonist, are key regulators of thymocyte migration and maturation in normal and inflammatory conditions. The specific agonist or ligand that binds CCR9 is CCL25 also referred to as TECK in some literature. The effects of chemokines binding to their specific receptors is generally dependent on the structural placement of the N terminal cysteine(s) amino acids. Receptors are broken down into 4 family groups CXC, CC, C, and CX3C, because CCR9 has two adjacent cysteines it is a C-C family receptor. C-C family chemokines (such as CCL25) are often associated with the recruitment of lymphocytes. It has been found that this gene is differentially expressed by T lymphocytes of small intestine and colon, suggesting a role in thymocyte recruitment and development that may permit functional specialization of immune responses in different segments of the gastrointestinal tract.
Clinical significance
The breadth of effects following interactions of CCR9 and |
https://en.wikipedia.org/wiki/Neuropeptide%20FF%20receptor%202 | Neuropeptide FF receptor 2, also known as NPFF2 is a human protein encoded by the NPFFR2 gene.
See also
Neuropeptide FF receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Prokineticin%20receptor%201 | Prokineticin receptor 1, also known as PKR1, is a human protein encoded by the PROKR1 gene.
See also
Prokineticin receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR75 | Probable G-protein coupled receptor 75 is a protein that in humans is encoded by the GPR75 gene.
Function
GPR75 is a member of the G protein-coupled receptor family. GPRs are cell surface receptors that activate guanine-nucleotide binding proteins upon the binding of a ligand.
GPR75 is currently classified as an orphan GPCR and several studies are underway to identify its ligand. In one study, the chemokine CCL5 (RANTES) has been shown to stimulate calcium mobilization and inositol triphosphate formation in GPR75-transfected cells.
A 2021 study reported that people with protein-truncating variants of GPR75 were associated with 5.3kg lower body weight and 54% lower odds for obesity. GPR75 knock-out mice showed resistance to weight gain under high-fat diet.
References
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Frizzled-10 | Frizzled-10 (Fz-10) is a protein that in humans is encoded by the FZD10 gene. Fz-10 has also been designated as CD350 (cluster of differentiation 350).
Function
This gene is a member of the frizzled gene family. Members of this family encode 7-transmembrane domain proteins that are receptors for the Wingless type MMTV integration site family of signaling proteins. Most frizzled receptors are coupled to the beta-catenin canonical signaling pathway. Using array analysis, expression of this intronless gene is significantly up-regulated in two cases of primary colon cancer.
References
Further reading
External links
Clusters of differentiation
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR45 | Probable G-protein coupled receptor 45 is a protein that in humans is encoded by the GPR45 gene.
This intronless gene encodes a member of the G protein-coupled receptor (GPCR) family. Members of this protein family contain seven putative transmembrane domains and may mediate signaling processes to the interior of the cell via activation of heterotrimeric G proteins. This protein may function in the central nervous system.
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Prostaglandin%20DP2%20receptor | {{DISPLAYTITLE:Prostaglandin DP2 receptor}}
Prostaglandin D2 receptor 2 (DP2 or CRTH2) is a human protein encoded by the PTGDR2 gene and GPR44. DP2 has also been designated as CD294 (cluster of differentiation 294). It is a member of the class of prostaglandin receptors which bind with and respond to various prostaglandins. DP2 along with Prostaglandin DP1 receptor are receptors for prostaglandin D2 (PGD2). Activation of DP2 by PGD2 or other cognate receptor ligands has been associated with certain physiological and pathological responses, particularly those associated with allergy and inflammation, in animal models and certain human diseases.
Gene
The PTGDR2 gene is located on human chromosome 11 at position q12.2 (i.e. 11q12.2). It consists of two introns and three exons and codes for a G protein coupled receptor (GPCR) composed of 472 amino acids. DP2, is related to members of the chemotactic factor class of GPCRs, sharing an amino acid sequence identity of 29% with the C5a receptor, Formyl peptide receptor 1, and Formyl peptide receptor 2 receptors. DP2 has little or no such amino acid sequence relationship to the eight other Prostanoid receptors (see Eicosanoid receptor#Prostenoid receptors).
Expression
DP2 was found to stimulate the directed movement or chemotaxis of human T-helper type 2 cells (see T helper cell#Th1/Th2 Model for helper T cells) by binding to a receptor initially termed GPR44 and thereafter CRTH2 (for Chemoattractant Receptor-homologous molecule expr |
https://en.wikipedia.org/wiki/Latrophilin%201 | Latrophilin 1 is a protein that in humans is encoded by the ADGRL1 gene. It is a member of the adhesion-GPCR family of receptors. Family members are characterized by an extended extracellular region with a variable number of protein domains coupled to a TM7 domain via a domain known as the GPCR-Autoproteolysis INducing (GAIN) domain.
Function
This gene encodes a member of the latrophilin subfamily of G protein-coupled receptors (GPCR). Latrophilins may function in both cell adhesion and signal transduction. In experiments with non-human species, endogenous proteolytic cleavage within a cysteine-rich GPS (G-protein-coupled-receptor proteolysis site) domain resulted in two subunits (a large extracellular N-terminal cell adhesion subunit and a subunit with substantial similarity to the secretin/calcitonin family of GPCRs) being non-covalently bound at the cell membrane. Latrophilin-1 has been shown to recruit the neurotoxin from black widow spider venom, alpha-latrotoxin, to the synapse plasma membrane. Latrophilin-1 also binds glucose and possibly other carbohydrates because of its lectin domain. It may be involved in mediating glucose and energy balance as shown recently..
See also
Adhesion G protein-coupled receptors
References
Further reading
External links
PDBe-KB provides an overview of all the structure information available in the PDB for Mouse Adhesion G protein-coupled receptor L1
Latrophilins |
https://en.wikipedia.org/wiki/Latrophilin%203 | Latrophilin 3 is a protein that in humans is encoded by the ADGRL3 gene.
Function
This gene encodes a member of the latrophilin subfamily of G protein-coupled receptors (GPCR). Latrophilins may function in both cell adhesion and signal transduction. In experiments with non-human species, endogenous proteolytic cleavage within a cysteine-rich GPS (G-protein-coupled-receptor proteolysis site) domain resulted in two subunits (a large extracellular N-terminal cell adhesion subunit and a subunit with substantial similarity to the secretin/calcitonin family of GPCRs) being non-covalently bound at the cell membrane.
Clinical significance
A version of this gene has been linked to attention deficit hyperactivity disorder (ADHD).
See also
Adhesion G protein-coupled receptors
References
Further reading
External links
PDBe-KB provides an overview of all the structure information available in the PDB for Human Adhesion G protein-coupled receptor L3
PDBe-KB provides an overview of all the structure information available in the PDB for Mouse Adhesion G protein-coupled receptor L3
Latrophilins
Biology of attention deficit hyperactivity disorder |
https://en.wikipedia.org/wiki/OPN3 | Opsin-3 also known as encephalopsin or panopsin is a protein that, in humans, is encoded by the OPN3 gene. Alternative splicing of this gene results in multiple transcript variants encoding different protein isoforms.
Function
Opsins are members of the G protein-coupled receptor superfamily. In addition to the visual opsins, mammals possess several photoreceptive non-visual opsins that are expressed in tissues outside the eye. The opsin-3 gene is strongly expressed in brain and testis and weakly expressed in liver, placenta, heart, lung, skeletal muscle, kidney, and pancreas. The gene is expressed in the skin and may also be expressed in the retina. The protein has the canonical features of a photoreceptive opsin protein, however in human skin, OPN3 is not photoreceptive and acts as a negative regulator of melanogenesis.
Applications
When OPN3 analogues are expressed in neurons, activation by light inhibits neurotransmitter release. This makes these analogues useful tools for optogenetic silencing, a method to study the impact of specific neurons on brain function.
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Neurotensin%20receptor%202 | Neurotensin receptor type 2 is a protein that in humans is encoded by the NTSR2 gene.
Function
The protein encoded by this gene belongs to the G protein-coupled receptor family that activates a phosphatidylinositol-calcium second messenger system. Binding and pharmacological studies demonstrate that this receptor binds neurotensin as well as several other ligands already described for neurotensin NT1 receptor. However, unlike NT1 receptor, this gene recognizes, with high affinity, levocabastine, a histamine H1 receptor antagonist previously shown to compete with neurotensin for low-affinity binding sites in the brain. These activities suggest that this receptor may be of physiological importance and that a natural agonist for the receptor may exist.
See also
Neurotensin receptor
References
Further reading
External links
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR124 | Probable G-protein coupled receptor 124 is a protein that in humans is encoded by the GPR124 gene. It is a member of the adhesion-GPCR family of receptors. Family members are characterized by an extended extracellular region with a variable number of protein domains coupled to a TM7 domain via a domain known as the GPCR-Autoproteolysis INducing (GAIN) domain.
Interactions
GPR124 has been shown to interact with DLG1 and is involved in the Wnt/β-catenin signaling pathway along with RECK.
Zebrafish embryos with Gpr124 loss of function demonstrate severe angiogenic deficiencies in the central nervous system.
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Ulinastatin | Ulinastatin, as an urinary trypsin inhibitor (UTI), is a glycoprotein that is isolated from healthy human urine or synthetically produced and has molecular weight of 25 - 40kDa. Highly purified ulinastatin has been clinically used for the treatment of acute pancreatitis, chronic pancreatitis, Stevens–Johnson syndrome, burns, septic shock, and toxic epidermal necrolysis (TEN).
The drug is used in Japan, where its brand name is Miraclid, as well as in South Korea, China, and India. In India, where it is approved to treat severe sepsis and acute pancreatitis, it is marketed under the brand name Ulihope, Ulicrit-Liquid, Ulinase,U-Tryp in India. It is also known by the names Bikunin and Urinastatin. In China, where it is approved to treat acute pancreatitis, chronic recurrent pancreatitis and acute circulatory failure, it is marketed under the brand name Techpool Roan.
Effectiveness
Ulinastatin is available in countries like China, Japan and India for the management of sepsis and acute pancreatitis.
In Japan, It is clinically used to treat endoscopic retrograde cholangiopancreatography (ERCP)-induced pancreatitis. Studies in Japan have documented a reduction in the incidence of ERCP-induced pancreatitis with the use of ulinastatin. In one study, the incidence of hyperenzymemia and pancreatitis was significantly lower in the ulinastatin group than in the placebo group. In another study, ulinastatin reduced serum, drain amylase, and the incidence of postoperative pancreatitis f |
https://en.wikipedia.org/wiki/Haor | A () is a wetland ecosystem in the north eastern part of Bangladesh which physically is a bowl or saucer shaped shallow depression, also known as a backswamp. During monsoon receive surface runoff water from rivers and canals to become vast stretches of turbulent water.
In Bangladesh and in the deltaic part of the Indian state of West Bengal, which lie in the floodplain of three great rivers, the Bengali language has several terms to differentiate between lakes, including , , and . All four are types of similar freshwater wetlands. The line of difference between a , a and a is usually very thin.
A is usually a depression or topographic low generally produced by erosion or other geographical process. These are marshy in character. Sometimes are remains of a river that has changed its course. Many of the dry up in the winter but during the rains expand into broad and shallow sheets of water, which may be described as fresh water lagoons. are generally smaller than , but there also are large like Chalan Beel in Rajshahi Division, through which the Atrai River passes. It has shrunk over the years but still occupies an area of 26 km2 in dry season. Sometimes small permanent water bodies within the remain after the dry up. These are also called , which occupy the lowest part of the depressions. A or is an oxbow lake, namely moribund beds of Bhairab, Kaliganga, Gorai and Kumar rivers.
A simple definition was provided by hydrologist Saila Parveen, " – seasonal wetlan |
https://en.wikipedia.org/wiki/Landau%E2%80%93Zener%20formula | The Landau–Zener formula is an analytic solution to the equations of motion governing the transition dynamics of a two-state quantum system, with a time-dependent Hamiltonian varying such that the energy separation of the two states is a linear function of time. The formula, giving the probability of a diabatic (not adiabatic) transition between the two energy states, was published separately by Lev Landau, Clarence Zener, Ernst Stueckelberg, and Ettore Majorana, in 1932.
If the system starts, in the infinite past, in the lower energy eigenstate, we wish to calculate the probability of finding the system in the upper energy eigenstate in the infinite future (a so-called Landau–Zener transition). For infinitely slow variation of the energy difference (that is, a Landau–Zener velocity of zero), the adiabatic theorem tells us that no such transition will take place, as the system will always be in an instantaneous eigenstate of the Hamiltonian at that moment in time. At non-zero velocities, transitions occur with probability as described by the Landau–Zener formula.
Conditions and approximation
Such transitions occur between states of the entire system, hence any description of the system must include all external influences, including collisions and external electric and magnetic fields. In order that the equations of motion for the system might be solved analytically, a set of simplifications are made, known collectively as the Landau–Zener approximation. The simplificatio |
https://en.wikipedia.org/wiki/Hilbert%E2%80%93Huang%20transform | The Hilbert–Huang transform (HHT) is a way to decompose a signal into so-called intrinsic mode functions (IMF) along with a trend, and obtain instantaneous frequency data. It is designed to work well for data that is nonstationary and nonlinear. In contrast to other common transforms like the Fourier transform, the HHT is an algorithm that can be applied to a data set, rather than a theoretical tool.
The Hilbert–Huang transform (HHT), a NASA designated name, was proposed by Norden E. Huang et al. (1996, 1998, 1999, 2003, 2012). It is the result of the empirical mode decomposition (EMD) and the Hilbert spectral analysis (HSA). The HHT uses the EMD method to decompose a signal into so-called intrinsic mode functions (IMF) with a trend, and applies the HSA method to the IMFs to obtain instantaneous frequency data. Since the signal is decomposed in time domain and the length of the IMFs is the same as the original signal, HHT preserves the characteristics of the varying frequency. This is an important advantage of HHT since a real-world signal usually has multiple causes happening in different time intervals. The HHT provides a new method of analyzing nonstationary and nonlinear time series data.
Definition
Empirical mode decomposition
The fundamental part of the HHT is the empirical mode decomposition (EMD) method. Breaking down signals into various components, EMD can be compared with other analysis methods such as Fourier transform and Wavelet transform. Using the EMD me |
https://en.wikipedia.org/wiki/PAR1 | PAR1 may refer to:
PAR1 (gene), Prader–Willi/Angelman region-1 gene
PAR-1, a serine/threonine-protein kinase of the KIN2/PAR-1/MARK kinase family
Coagulation factor II receptor
Parchive, a data archive format
PAR1, one of the pseudoautosomal regions of the X or Y chromosome |
https://en.wikipedia.org/wiki/S3%20Group | S3 Group is a technology company that has provided software products to operators, OEM's, semiconductors and healthcare providers. Founded in 1986 as Silicon & Software Systems (S3), S3 Group has a history in systems, embedded software and silicon design for consumer, wireless, WiMAX and related applications.
In 2015, the group's "S3 TV Technology" business unit was sold to Accenture, and in 2018, the "S3 Semiconductors" division sold to Adesto Technologies. The remaining "S3 Connected Health" unit had, as of 2018, approximately 200 employees.
References
External links
Companies based in Dublin (city) |
https://en.wikipedia.org/wiki/1973%E2%80%9374%20Winnipeg%20Jets%20season | The 1973–74 Winnipeg Jets season was their second season in the World Hockey Association (WHA).
Regular season
Season standings
Playoffs
Houston Aeros 4, Winnipeg Jets 0
Player statistics
Forwards
Note: GP= Games played; G= Goals; A= Assists; PTS = Points; PIM = Points
Defencemen
Note: GP= Games played; G= Goals; A= Assists; PTS = Points; PIM = Points
Goaltending
Note: GP= Games played; MIN= Minutes; W= Wins; L= Losses; T = Ties; SO = Shutouts; GAA = Goals against
Draft picks
Winnipeg's draft picks at the 1973 WHA Amateur Draft.
References
External links
Jets on Hockey Database
Winnipeg Jets (1972–1996) seasons
Winn
Winn |
https://en.wikipedia.org/wiki/Hyalomma | Hyalomma is a genus of hard-bodied ticks common in Asia, Europe, and North Africa. They are also found in Southern Africa. The name is derived from Greek: hyalos (ὕαλος) crystal, glass; and omma (oμμα) eye.
The genus is believed to have originated in Iran or Central Asia, and then spread further into Asia, including the Middle East, and to southern Europe and Africa.
Hyalomma are larger in size and do not have protective shields (indistinct festoons), but have eyes and banded legs. Hyalomma species are difficult to identify due to their hybridization and genetic and morphological variations, caused by harsh environmental conditions and lack of food sources. Hyalomma species are the only ticks to live in such harsh desert conditions. With few hosts available, they are required to be active as soon as a potential host is sensed.
Adult Hyalomma can bite humans and transmit serious pathogens. Immature (nymph) Hyalomma usually feed on birds, rodents, and hares and can be the cause of viral disease and rickettsias. Nymphs are often transmitted from one place to another by migrating birds. For example, a migrating bird carrying a Hyalomma marginatum nymph can cause Crimean-Congo hemorrhagic fever. Hyalomma species can also transmit rickettsias like Siberian tick typhus, Boutonneuse fever, and Q fever.
Species
Hyalomma aegyptium Linnaeus, 1758
Hyalomma albiparmatum Schulze, 1919
Hyalomma anatolicum, parasite of camel
Hyalomma anatolicum excavatum
Hyalomma arabica Pegram, Hoo |
https://en.wikipedia.org/wiki/PRKAR1A | cAMP-dependent protein kinase type I-alpha regulatory subunit is an enzyme that in humans is encoded by the PRKAR1A gene.
Function
cAMP is a signaling molecule important for a variety of cellular functions. cAMP exerts its effects by activating the cAMP-dependent protein kinase A (PKA), which transduces the signal through phosphorylation of different target proteins. The inactive holoenzyme of PKA is a tetramer composed of two regulatory and two catalytic subunits. cAMP causes the dissociation of the inactive holoenzyme into a dimer of regulatory subunits bound to four cAMP and two free monomeric catalytic subunits. Four different regulatory subunits and three catalytic subunits of PKA have been identified in humans. The protein encoded by this gene is one of the regulatory subunits. This protein was found to be a tissue-specific extinguisher that down-regulates the expression of seven liver genes in hepatoma x fibroblast hybrids Three alternatively spliced transcript variants encoding the same protein have been observed.
Clinical significance
Functional null mutations in this gene cause Carney complex (CNC), an autosomal dominant multiple neoplasia syndrome. This gene can fuse to the RET protooncogene by gene rearrangement and form the thyroid tumor-specific chimeric oncogene known as PTC2.
Mutation of PRKAR1A leads to the Carney complex, associating multiple endocrine tumors.
Interactions
PRKAR1A has been shown to interact with:
AKAP10,
AKAP1,
AKAP4,
ARFGE |
https://en.wikipedia.org/wiki/Environment%20of%20Brazil | The environment of Brazil is characterized by high biodiversity with a population density that decreases away from the coast.
Brazil's large area comprises different ecosystems, which together sustain some of the world's greatest biodiversity. Because of the country's intense economic and demographic growth, Brazil's ability to protect its environmental habitats has increasingly come under threat.
Extensive legal and Illegal logging destroys forests the size of a small country per year, and with it a diverse series of species through habitat destruction and habitat fragmentation. Between 2002 and 2006, an area of the Amazon Rainforest equivalent in size to the State of South Carolina was completely deforested for the purposes of raising cattle and woodlogging. In April 2012 Brazil's powerful farm lobby won a long-sought victory after the National Congress of Brazil approved a controversial forestry bill that environmentalists say will speed deforestation in the Amazon as more land is opened for producing food. By 2020, at least 50% of the species resident in Brazil may become extinct.
There is a general consensus that Brazil has the highest number of both terrestrial vertebrates and invertebrates of any single country in the world. Also, Brazil has the highest primate diversity, the highest number of mammals, the highest number of amphibians, the second highest number of butterflies, the third highest number of birds, and second highest number of reptiles. There is a hi |
https://en.wikipedia.org/wiki/Fluid%20compartments | The human body and even its individual body fluids may be conceptually divided into various fluid compartments, which, although not literally anatomic compartments, do represent a real division in terms of how portions of the body's water, solutes, and suspended elements are segregated. The two main fluid compartments are the intracellular and extracellular compartments. The intracellular compartment is the space within the organism's cells; it is separated from the extracellular compartment by cell membranes.
About two-thirds of the total body water of humans is held in the cells, mostly in the cytosol, and the remainder is found in the extracellular compartment. The extracellular fluids may be divided into three types: interstitial fluid in the "interstitial compartment" (surrounding tissue cells and bathing them in a solution of nutrients and other chemicals), blood plasma and lymph in the "intravascular compartment" (inside the blood vessels and lymphatic vessels), and small amounts of transcellular fluid such as ocular and cerebrospinal fluids in the "transcellular compartment".
The normal processes by which life self-regulates its biochemistry (homeostasis) produce fluid balance across the fluid compartments. Water and electrolytes are continuously moving across barriers (eg, cell membranes, vessel walls), albeit often in small amounts, to maintain this healthy balance. The movement of these molecules is controlled and restricted by various mechanisms. When illness |
https://en.wikipedia.org/wiki/Suppressor%20of%20cytokine%20signaling%201 | Suppressor of cytokine signaling 1 is a protein that in humans is encoded by the SOCS1 gene. SOCS1 orthologs have been identified in several mammals for which complete genome data are available.
Function
This gene encodes a member of the STAT-induced STAT inhibitor (SSI), also known as suppressor of cytokine signalling (SOCS), family. SSI family members are cytokine-inducible negative regulators of cytokine signaling. The expression of this gene can be induced by a subset of cytokines, including IL2, IL3 erythropoietin (EPO), GM-CSF, and interferon-gamma (IFN-γ). The protein encoded by this gene functions downstream of cytokine receptors, and takes part in a negative feedback loop to attenuate cytokine signaling. Knockout studies in mice suggested the role of this gene as a modulator of IFN-γ action, which is required for normal postnatal growth and survival.
Several recent viral studies have shown that viral genes, such as Tax gene product (Tax), encoded by HTLV-1, could hijack SOCS1 to inhibit host antiviral pathways, as a strategy to evade host immunity.
Interactions
The suppressor of cytokine signaling 1 has been shown to interact with:
Tax,
CD117,
Colony stimulating factor 1 receptor
Growth hormone receptor,
IRS2,
Janus kinase 2, and
TEC.
See also
SOCS
JAK-STAT signaling pathway
References
Further reading
Cell signaling
Signal transduction |
https://en.wikipedia.org/wiki/STK11 | Serine/threonine kinase 11 (STK11) also known as liver kinase B1 (LKB1) or renal carcinoma antigen NY-REN-19 is a protein kinase that in humans is encoded by the STK11 gene.
Expression
Testosterone and DHT treatment of murine 3T3-L1 or human SGBS adipocytes for 24 h significantly decreased the mRNA expression of LKB1 via the androgen receptor and consequently reduced the activation of AMPK by phosphorylation. In contrast, 17β-estradiol treatment increased LKB1 mRNA, an effect mediated by oestrogen receptor alpha.
However, in ER-positive breast cancer cell line MCF-7, estradiol caused a dose-dependent decrease in LKB1 transcript and protein expression leading to a significant decrease in the phosphorylation of the LKB1 target AMPK. ERα binds to the STK11 promoter in a ligand-independent manner and this interaction is decreased in the presence of estradiol. Moreover, STK11 promoter activity is significantly decreased in the presence of estradiol.
Function
The STK11/LKB1 gene, which encodes a member of the serine/threonine kinase family, regulates cell polarity and functions as a tumour suppressor.
LKB1 is a primary upstream kinase of adenosine monophosphate-activated protein kinase (AMPK), a necessary element in cell metabolism that is required for maintaining energy homeostasis. It is now clear that LKB1 exerts its growth suppressing effects by activating a group of ~14 other kinases, comprising AMPK and AMPK-related kinases. Activation of AMPK by LKB1 suppresses growth a |
https://en.wikipedia.org/wiki/Spindle%20cell%20sarcoma | Spindle cell sarcoma is a type of connective tissue cancer . The tumors generally begin in layers of connective tissue, as found under the skin, between muscles, and surrounding organs, and will generally start as a small, inflamed lump, which grows in size. At first, the lump is, small in size, as the tumor exists in stage 1, and will not necessarily expand beyond its encapsulated form. However, it may develop cancerous traits that can only be detected through microscopic examination or cell-level molecular analysis. As such, at Stage 1, the tumor is usually treated by excision, which includes wide margins of healthy-looking tissue, followed by thorough biopsy, and additional excision, if necessary. The prognosis for a stage 1 tumor excision is usually fairly optimistic, but if the tumor progresses to levels 2 and 3, prognosis worsens, due to tumor cells' likely having spread to other parts of the body, including nearby healthy tissues, or to system-wide locations that include the lungs, kidneys, and liver. In these cases, prognosis is grim and chemotherapy and radiation are the only methods of controlling the cancer.
A variety of factors influence the incidence of spindle cell sarcoma, including genetic predisposition, but it may also be caused by a combination of other factors, including injury and inflammation in patients who are already thought to be predisposed to such tumors. Normal spindle cells are a naturally occurring part of the body's response to injury. In res |
https://en.wikipedia.org/wiki/Amiga%20productivity%20software | This article deals with productivity software created for the Amiga line of computers and covers the AmigaOS operating system and its derivatives AROS and MorphOS. It is a split of the main article, Amiga software.
History
The Amiga originally supported such prestigious software titles as WordPerfect, Electronic Arts' Deluxe Paint, and Lattice C. Newtek's Video Toaster, one of the first all-in-one graphics and video editing packages, began on the Amiga. The Video Toaster was one of the few accessories for the "big box" Amigas (2000, 3000 and 4000) that used the video slot and enabled users to turn their Amiga into the heart of an entire TV production suite. The later addition of the Video Flyer by Newtek made possible the first non-linear video editing program for the Amiga. The Amiga made 3D raytracing graphics available for the masses with Sculpt 3D. Before the Amiga, raytracing was only available for dedicated graphic workstations such as the SGI. Other raytracing software also included TurboSilver. The Amiga was well known for its 3D rendering capability, with many titles being added to the mix as the years went by. Some titles were later ported to Microsoft Windows and continue to thrive there, such as the rendering software Cinema 4D from Maxon, and LightWave from Newtek, which was originally part of the Video Toaster. The Video Toaster itself has even been ported to the Windows platform. LightWave was used for low-cost computer generated special effects during the e |
https://en.wikipedia.org/wiki/TAF1 | Transcription initiation factor TFIID subunit 1, also known as transcription initiation factor TFIID 250 kDa subunit (TAFII-250) or TBP-associated factor 250 kDa (p250), is a protein that in humans is encoded by the TAF1 gene.
Function
Initiation of transcription by RNA polymerase II requires the activities of more than 70 polypeptides. The protein that coordinates these activities is the basal transcription factor TFIID, which binds to the core promoter to position the polymerase properly, serves as the scaffold for assembly of the remainder of the transcription complex, and acts as a channel for regulatory signals. TFIID is composed of the TATA-binding protein (TBP) and a group of evolutionarily conserved proteins known as TBP-associated factors or TAFs. TAFs may participate in basal transcription, serve as coactivators, function in promoter recognition or modify general transcription factors (GTFs) to facilitate complex assembly and transcription initiation. This gene encodes the largest subunit of TFIID. This subunit binds to core promoter sequences encompassing the transcription start site. It also binds to activators and other transcriptional regulators, and these interactions affect the rate of transcription initiation. This subunit contains two independent protein kinase domains at the N and C-terminals, but also possesses acetyltransferase activity and can act as a ubiquitin-activating/conjugating enzyme. Two transcripts encoding different isoforms have been identi |
https://en.wikipedia.org/wiki/Adiabatic%20quantum%20computation | Adiabatic quantum computation (AQC) is a form of quantum computing which relies on the adiabatic theorem to perform calculations and is closely related to quantum annealing.
Description
First, a (potentially complicated) Hamiltonian is found whose ground state describes the solution to the problem of interest. Next, a system with a simple Hamiltonian is prepared and initialized to the ground state. Finally, the simple Hamiltonian is adiabatically evolved to the desired complicated Hamiltonian. By the adiabatic theorem, the system remains in the ground state, so at the end, the state of the system describes the solution to the problem. Adiabatic quantum computing has been shown to be polynomially equivalent to conventional quantum computing in the circuit model.
The time complexity for an adiabatic algorithm is the time taken to complete the adiabatic evolution which is dependent on the gap in the energy eigenvalues (spectral gap) of the Hamiltonian. Specifically, if the system is to be kept in the ground state, the energy gap between the ground state and the first excited state of provides an upper bound on the rate at which the Hamiltonian can be evolved at time When the spectral gap is small, the Hamiltonian has to be evolved slowly. The runtime for the entire algorithm can be bounded by:
where is the minimum spectral gap for
AQC is a possible method to get around the problem of energy relaxation. Since the quantum system is in the ground state, interference with th |
https://en.wikipedia.org/wiki/Dopamine%20receptor%20D3 | {{DISPLAYTITLE:Dopamine receptor D3}}
Dopamine receptor D3 is a protein that in humans is encoded by the DRD3 gene.
This gene encodes the D3 subtype of the dopamine receptor. The D3 subtype inhibits adenylyl cyclase through inhibitory G-proteins. This receptor is expressed in phylogenetically older regions of the brain, suggesting that this receptor plays a role in cognitive and emotional functions. It is a target for drugs which treat schizophrenia, drug addiction, and Parkinson's disease. Alternative splicing of this gene results in multiple transcript variants that would encode different isoforms, although some variants may be subject to nonsense-mediated decay (NMD).
Function
Alpha-synuclein (α-Syn) aggregation via Lewy bodies inclusion, a pathogenic signature exclusively present in PD patients, is decreased by D3 agonists while DA content is elevated by inhibiting DA reuptake and breakdown. The regulation of α-Syn aggregation and clearance enhances brain-derived neurotrophic factor (BDNF) secretion, which ultimately ameliorates neuroinflammation and oxidative stress while promoting neurogenesis and interacting with other DA receptors.
D3 agonists like 7-OH-DPAT, pramipexole, and rotigotine, among others, display antidepressant effects in rodent models of depression. Apomorphine has the ability to help PD patients with their cognition awareness. In addition to having antidepressant properties such as regulating the depression-like behaviors and depression developmen |
https://en.wikipedia.org/wiki/Death%20receptor%205 | Death receptor 5 (DR5), also known as TRAIL receptor 2 (TRAILR2) and tumor necrosis factor receptor superfamily member 10B (TNFRSF10B), is a cell surface receptor of the TNF-receptor superfamily that binds TRAIL and mediates apoptosis.
Function
The protein encoded by this gene is a member of the TNF-receptor superfamily, and contains an intracellular death domain. This receptor can be activated by tumor necrosis factor-related apoptosis inducing ligand (TNFSF10/TRAIL/APO-2L), and transduces apoptosis signal. Mice have a homologous gene, tnfrsf10b, that has been essential in the elucidation of the function of this gene in humans. Studies with FADD-deficient mice suggested that FADD, a death domain containing adaptor protein, is required for the apoptosis mediated by this protein.
Interactions
DR5 has been shown to interact with:
Caspase 8,
Caspase 10,
FADD, and
TRAIL.
Cancer therapy
Monoclonal antibodies targeting DR5 have been developed and are currently under clinical trials for patients suffer from a variety of cancer types, see Tigatuzumab (CS-1008).
Luminescent iridium complex-peptide hybrids, serving as TRAIL mimics, have been designed, which target the death receptors DR4 and DR5 on cancer cells and induce their apoptosis.
See also
Cluster of differentiation
Tumor necrosis factor receptor
Tigatuzumab
References
Further reading
External links
Clusters of differentiation
TNF receptor family |
https://en.wikipedia.org/wiki/Cannabinoid%20receptor%201 | Cannabinoid receptor 1 (CB1), is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene. The human CB1 receptor is expressed in the peripheral nervous system and central nervous system. It is activated by endocannabinoids, a group of retrograde neurotransmitters that include anandamide and 2-arachidonoylglycerol (2-AG); plant phytocannabinoids, such as docosatetraenoylethanolamide found in wild daga, the compound THC which is an active constituent of the psychoactive drug cannabis; and synthetic analogs of THC. CB1 is antagonized by the phytocannabinoid tetrahydrocannabivarin (THCV).
The primary endogenous agonist of the human CB1 receptor is anandamide.
Structure
The CB1 receptor shares the structure characteristic of all G-protein-coupled receptors, possessing seven transmembrane domains connected by three extracellular and three intracellular loops, an extracellular N-terminal tail, and an intracellular C-terminal tail. The receptor may exist as a homodimer or form heterodimers or other GPCR oligomers with different classes of G-protein-coupled receptors. Observed heterodimers include A2A–CB1, CB1–D2, OX1–CB1, μOR–CB1, while many more may only be stable enough to exist in vivo. The CB1 receptor possesses an allosteric modulatory binding site.
Mechanism
The CB1 receptor is a pre-synaptic heteroreceptor that modulates neurotransmitter release when activated in a dose-dependent, stereoselective and pertussis toxin-sensitive manner. The CB1 rec |
https://en.wikipedia.org/wiki/Cannabinoid%20receptor%202 | The cannabinoid receptor 2 (CB2), is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the CNR2 gene. It is closely related to the cannabinoid receptor 1 (CB1), which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic-inhibition, the psychoactive properties of tetrahydrocannabinol (THC), the active agent in cannabis, and other phytocannabinoids (plant cannabinoids). The principal endogenous ligand for the CB2 receptor is 2-Arachidonoylglycerol (2-AG).
CB2 was cloned in 1993 by a research group from Cambridge looking for a second cannabinoid receptor that could explain the pharmacological properties of tetrahydrocannabinol. The receptor was identified among cDNAs based on its similarity in amino-acid sequence to the cannabinoid receptor 1 (CB1) receptor, discovered in 1990. The discovery of this receptor helped provide a molecular explanation for the established effects of cannabinoids on the immune system.
Structure
The CB2 receptor is encoded by the CNR2 gene. Approximately 360 amino acids comprise the human CB2 receptor, making it somewhat shorter than the 473-amino-acid-long CB1 receptor.
As is commonly seen in G protein-coupled receptors, the CB2 receptor has seven transmembrane spanning domains, a glycosylated N-terminus, and an intracellular C-terminus. The C-terminus of CB2 receptors appears to play a critical role in the regulation of ligand-induced receptor desensitization and downregul |
https://en.wikipedia.org/wiki/World%20Christian%20Encyclopedia | World Christian Encyclopedia is a reference work, with its third edition published by Edinburgh University Press in November 2019. The WCE is known for providing membership statistics for major world religions and Christian denominations including historical data and projections of future populations.
The data incorporated into the World Christian Encyclopedia have been made available online at the World Christian Database (WCD).
Editions
1st - 1982
The first edition, World Christian Encyclopedia: A Comparative Survey of Churches and Religions in the Modern World A.D. 1900–2000 (WCE), by David B. Barrett, was published in 1982 by Oxford University Press. Barrett was a trained aeronautical engineer who became a missionary with the Church Missionary Society (Anglican). He arrived in Nyanza Province in Western Kenya in 1957. Over the course of 14 years he traveled to 212 of 223 countries and corresponded with Christians all over the world in search of the most up-to-date statistics on Christianity and world religions. His research resulted in the first edition of the World Christian Encyclopedia in 1982.
2nd - 2001
Barrett moved to Richmond, Virginia in 1985 to work with the Southern Baptists on missionary strategy. He continued his research as an independent researcher, joined by Todd M. Johnson in 1988. With George Kurian, Barrett and Johnson produced the second edition of the World Christian Encyclopedia, in 2 volumes, in 2001 (Oxford University Press).
3rd - 2019
The th |
https://en.wikipedia.org/wiki/GPR160 | Probable G-protein coupled receptor 160 is a protein that in humans is encoded by the GPR160 gene.
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/GPR82 | Probable G-protein coupled receptor 82 is a protein that in humans is encoded by the GPR82 gene.
G protein-coupled receptors (GPCRs, or GPRs) contain 7 transmembrane domains and transduce extracellular signals through heterotrimeric G proteins.[supplied by OMIM]
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/Hydroxycarboxylic%20acid%20receptor%201 | Hydroxycarboxylic acid receptor 1 (HCA1), formerly known as G protein-coupled receptor 81 (GPR81), is a protein that in humans is encoded by the HCAR1 gene. HCA1, like the other hydroxycarboxylic acid receptors HCA2 and HCA3, is a G protein-coupled receptor (GPCR). The primary endogenous agonist of HCA1 is lactic acid (and its conjugate base, lactate).
Lactate was initially found to activate HCA1 on fat cells and thereby to inhibit these cells lipolysis i.e., break-down of their fats into free fatty acids and glycerol. Subsequent studies have found that in addition to fat cells, HCA1 is expressed on cells in the brain, skeletal muscle, lymphoid tissue, uterus, kidney, liver, and pancreas as well as on immune cells such as macrophages and antigen-presenting cells. In the brain, HCA1 acts to dampen neuron excitation and may also function to promote neurogenesis (i.e., production of neurons from neural stem cells) and angiogenesis, i.e., formation of new blood vessels from pre-existing blood vessels). The functions of HCA1 in non-fat and non-neural tissues have not been fully defined but in many cases appear to involve promoting the survival of cells, including various types of cancer cells.
References
Further reading
G protein-coupled receptors |
https://en.wikipedia.org/wiki/OXGR1 | 2-Oxoglutarate receptor 1 (OXGR1), also known as cysteinyl leukotriene receptor E (CysLTE) and GPR99, is a protein that in humans is encoded by the (also termed GPR99) gene. The Gene has recently been nominated as a receptor not only for 2-oxogluterate (see alpha-Ketoglutaric acid) but also for the three cysteinyl leukotrienes (CysLTs), particularly leukotriene E4 (LTE4) and to far lesser extents LTC4 and LTE4. Recent studies implicate GPR99 as a cellular receptor which is activated by LTE4 thereby causing these cells to contribute to mediating various allergic and hypersensitivity responses.
History
In 2001, a gene projected to code for a G protein-like receptor protein was reported; the gene's apparent protein product was classified as an orphan receptor (i.e., a receptor whose activating ligand and function were unknown) and named GPR80. The projected amino acid sequence of the protein encoded by the GPR80 gene bore similarities to a purinergic receptor, P2Y1, and therefore might, like P2Y1, be a receptor for purine compounds. Shortly thereafter, a second report found this same gene, indicated that it coded for a G protein receptor with its amino acid sequence similarities closest to purinergic receptors GPR91 and P2Y1, and named the gene and its protein GPR99 and GPR99, respectively. While the latter report found that a large series of purinergic nucleotides, other nucleotides, and derivatives of these compounds did not activate GPR99-bearing cells, a third report in 2 |
https://en.wikipedia.org/wiki/GPR78 | Probable G-protein coupled receptor 78 is a protein that in humans is encoded by the GPR78 gene.
G protein-coupled receptors (GPCRs, or GPRs) contain 7 transmembrane domains and transduce extracellular signals through heterotrimeric G proteins.[supplied by OMIM]
References
Further reading
G protein-coupled receptors |
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