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12161402 | Influence of grapefruit juice on itraconazole plasma levels in mice and guinea pigs. | Levels of itraconazole and its metabolite hydroxy-itraconazole were measured by HPLC in plasma samples from guinea pigs and DBA/2 and BALB/c mice after oral or intraperitoneal treatment with itraconazole/cyclodextrin solution at 5 and 20 mg/kg daily for 7 days. The animals were randomly assigned to receive grapefruit j... |
12160414 | Routes to regioselective deuteriation of heteroaromatic compounds. | A systematic approach to the deuteriation of polypyridyl type ligands is reported. A range of isotopologues of heteroaromatic compounds containing pyrazyl, pyridyl, 1,2,4-triazole, thienyl, methyl, and phenyl moieties, have been prepared in a cost-effective manner, using a range of methods based on subcritical aqueous ... |
12160393 | Synthesis, structure, and DNA cleavage activity of new trinuclear Zn(3) and Zn(2)Cu complexes of a chiral macrocycle: structural correlation with the active center of P1 nuclease. | New homo trinuclear Zn(II) complexes [Zn(3)L(1)(micro-OAc)](ClO(4))(2).3CHCl(3).H(2)O, 1, and [Zn(3)L(1)(micro-OAc)].ClO(4).PF(6).5CH(3)OH.H(2)O, 2, and hetero trinuclear complex [Zn(2)CuL(1)(micro-OAc)](ClO(4))(2).3CHCl(3).H(2)O,3, of optically active hexaaza triphenolic macrocycle H(3)L(1) were synthesized and crysta... |
12153286 | Methylene-bridged glycoluril dimers: synthetic methods. | Methylene-bridged glycoluril dimers are the fundamental building blocks of cucurbituril (CB[6]), its homologues (CB[n]), and its derivatives. This paper describes three complementary methods for the synthesis of C- and S-shaped methylene-bridged glycoluril dimers (29-34 and 37-44). For this purpose, we prepared glycolu... |
12153280 | Supramolecular effects on the dynamics of radicals in MFI zeolites: a direct EPR investigation. | Photolysis of the supramolecular complexes (dibenzyl ketones@ZSM-5) produced supramolecular complexes of benzyl radicals@ZSM-5, which were directly detected by CW-EPR spectroscopy, and provided information on the dynamics of the radicals. The lifetimes of the radicals increased as the group X attached to the carbon ato... |
12153263 | 5,10,15-Triaryl-21,23-dioxacorrole and its isomer with a protruding furan ring. | An oxa-analogue of 5,10,15-triarylcorrole, i.e., 5,10,15-triaryl-21,23-dioxacorrole (21,23-O(2)Cor)H, where two pyrrole rings are replaced by furan moieties, has been produced by condensation of 2,5-bis(arylhydroxymethyl)furan, 2-phenylhydroxymethylfuran, and pyrrole. 2-Phenylhydroxymethylfuran serves as the suitable s... |
12153567 | The role of amino-acid residues Q39 and E451 in the determination of substrate specificity of the Spodoptera frugiperda beta-glycosidase. | The design of beta-glycosidases with planed substrate specificity for biotechnological application has received little attention. This is mostly a consequence of the lack of data on the molecular basis of the beta-glycosidase specificity, namely data on the energy of the noncovalent interactions in the enzyme-transitio... |
12151553 | Differential activation of orexin neurons by antipsychotic drugs associated with weight gain. | Weight gain is one side effect of many antipsychotic drugs (APDs). A small number of lateral hypothalamic/perifornical area (LH/PFA) neurons express the orexins, peptides that are critically involved in body weight regulation and arousal. We examined the ability of APDs to activate orexin neurons, as reflected by induc... |
12150703 | Considerations and development of topical microbicides to inhibit the sexual transmission of HIV. | The increased incidence of HIV/AIDS disease in women aged 15 - 49 years has identified the urgent need for a female-controlled, efficacious and safe vaginal topical microbicide. To meet this challenge, new topical microbicide candidates consisting of molecules or formulations that modify the genital environment (Buffer... |
12151211 | Synthesis of novel cyclomaltoheptaose (beta-cyclodextrin) derivatives containing the Ebselen key moiety of benzoisoselenazolone. | A series of five novel cyclomaltoheptaose (beta-cyclodextrin) derivatives containing benzoisoselenazolone groups have been synthesized as glutathione peroxidase mimics. |
12151209 | Effects of cellulase on the modification of cellulose. | Multicomponent cellulases, purified endoglucanases and cellobiohydrolases were assayed and shown to modify pure natural cellulose (softwood pulp). Changes in structure and properties of the cellulose caused by enzymatic treatment depend on the composition, the type of enzyme, and the treatment conditions. The reactivit... |
12149275 | Control of P2X(2) channel permeability by the cytosolic domain. | ATP-gated P2X channels are the simplest of the three families of transmitter-gated ion channels. Some P2X channels display a time- and activation-dependent change in permeability as they undergo the transition from the relatively Na(+)-selective I(1) state to the I(2) state, which is also permeable to organic cations. ... |
12149338 | Nasopharyngeal carriage of potential bacterial pathogens related to day care attendance, with special reference to the molecular epidemiology of Haemophilus influenzae. | Nasopharyngeal carriage of Haemophilus influenzae, Streptococcus pneumoniae, and Moraxella catarrhalis was studied in 259 children attending day care centers (DCC) in Amsterdam, The Netherlands, and in 276 control children. The DCC children were sampled a second time after 4 weeks. Carriage rates for DCC children and c... |
12149016 | Amphiphilic hairy disks with branched hydrophilic tails and a hexa-peri-hexabenzocoronene core. | Amphiphilic discotic molecules with hydrophilic side branches consisting of hexaphenyl hexa-peri-hexabenzocoronene and hexabiphenyl hexa-peri-hexabiphenylcoronene as the aromatic core and hexa-substituted oligoethers as the branched peripheral chains have been synthesized, and their microstructure has been characterize... |
12149014 | Structure and dynamics of metallomacrocycles: recognition of zinc xylyl-bicyclam by an HIV coreceptor. | As platforms for the design of metal-based therapeutic and diagnostic agents, macrocycles are rigid enough to provide strong metal binding sites and orient functional groups stereoselectively, yet flexible enough to accommodate structural changes required for induced-fit recognition of biological targets. We consider t... |
12148992 | Supramolecular assembly on surfaces: manipulating conductance in noncovalently modified mesoscale structures. | Molecules capable of complementary hydrogen bonding were used to control the noncovalent self-assembly and electronic properties of a chemically well-defined surface mesostructure. In this work, we patterned a footprint region for molecular assembly on a surface and used moieties featuring complementary recognition to ... |
12148985 | Synthetic hydraphile channels of appropriate length kill Escherichia coli. | Crown ether-based synthetic cation conducting channels called hydraphiles show clear ionophoretic activity in phospholipid vesicles. These compounds are shown to be active against the bacterium E. coli. Disk diffusion assays were performed to assess the toxicity of different hydraphile derivatives. Liquid culture tests... |
12149231 | Lactosylceramide-enriched glycosphingolipid signaling domain mediates superoxide generation from human neutrophils. | This study is focused on the functional significance of neutrophil lactosylceramide (LacCer)-enriched microdomains, which are involved in the initiation of a signal transduction pathway leading to superoxide generation. Treatment of neutrophils with anti-LacCer antibody, T5A7 or Huly-m13, induced superoxide generation ... |
12146974 | Key determinants of receptor activation in the agr autoinducing peptides of Staphylococcus aureus. | Staphylococcal pathogenesis is regulated by a two-component quorum-sensing system, agr, activated upon binding of a self-coded autoinducing peptide (AIP) to the receptor-histidine kinase, AgrC. The AIPs consist of a thiolactone macrocyle and an exocyclic "tail", both of which are important for function. In this report,... |
12147464 | Plasmid-borne genes code for an angular dioxygenase involved in dibenzofuran degradation by Terrabacter sp. strain YK3. | The genes responsible for angular dioxygenation of dibenzofuran in actinomycetes were cloned by using a degenerate set of PCR primers designed by using conserved sequences of the dioxygenase alpha subunit genes. One sequence of alpha subunit genes was commonly amplified from four dibenzofuran-utilizing actinomycetes: T... |
12144782 | Blocking transcription through a nucleosome with synthetic DNA ligands. | Pyrrole-imidazole (Py-Im) polyamides are synthetic ligands that bind in the minor groove of DNA. Previous studies have established that sites on nucleosomal DNA facing away from the histone octamer, or even partially facing the histone octamer, are fully accessible for molecular recognition by Py-Im polyamides, and tha... |
12145216 | Ordered assembly of the V(D)J synaptic complex ensures accurate recombination. | Recombination of gene segments at the immunoglobulin and T-cell receptor loci requires that the RAG1 and RAG2 proteins bring together DNA signal sequences (RSSs) with 12- and 23-bp spacers into a synaptic complex and cleave the DNA. A RAG1/2 multimer that can cleave both signals is shown to assemble on an isolated RSS,... |
12145099 | Glibenclamide binding to sulphonylurea receptor subtypes: dependence on adenine nucleotides. | 1: ATP-sensitive K(+) channels are composed of pore-forming subunits Kir6.2 and of sulphonylurea receptors (SURs); the latter are the target of the hypoglycaemic sulphonylureas like glibenclamide. Here, we report on the negative allosteric modulation by MgATP and MgADP of glibenclamide binding to SUR1 and to SUR2 mutan... |
12142447 | Folding and stability of the ligand-binding domain of the glucocorticoid receptor. | A complex pathway involving many molecular chaperones has been proposed for the folding, assembly, and maintenance of a high-affinity ligand-binding form of steroid receptors in vivo, including the glucocorticoid receptor. To better understand this intricate folding and assembly process, we studied the folding of the l... |
12142446 | Stable self-assembly of a protein engineering scaffold on gold surfaces. | The outer membrane protein OmpF from Escherichia coli is a member of a large family of beta-barrel membrane proteins. Some, like OmpF, are pore-forming proteins whilse others are active transporters or enzymes. We have previously shown that the receptor-binding domain (R-domain) of the toxin colicin N binds with high a... |
12142422 | Role of the C-terminal domain of the alpha subunit of RNA polymerase in LuxR-dependent transcriptional activation of the lux operon during quorum sensing. | During quorum sensing in Vibrio fischeri, the luminescence, or lux, operon is regulated in a cell density-dependent manner by the activator LuxR in the presence of an acylated homoserine lactone autoinducer molecule [N-(3-oxohexanoyl) homoserine lactone]. LuxR, which binds to the lux operon promoter at a position cente... |
12140339 | Characterisation of the DNA-binding profile of barley HvCBF1 using an enzymatic method for rapid, quantitative and high-throughput analysis of the DNA-binding activity. | A rapid and quantitative DNA-binding assay was developed based on the translational fusion of a DNA-binding protein (DBP) with a Neocallimastix patriciarum beta-1,4-D-glucanase, CelD. CelD releases a fluorescent 4-methylumbelliferyl product from 4-methylumbelliferyl cellobioside. This hydrolysis activity was used to qu... |
12139929 | Using orthologous and paralogous proteins to identify specificity-determining residues in bacterial transcription factors. | Concepts of orthology and paralogy are become increasingly important as whole-genome comparison allows their identification in complete genomes. Functional specificity of proteins is assumed to be conserved among orthologs and is different among paralogs. We used this assumption to identify residues which determine spe... |
12139454 | Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists. | A series of tricyclic imidazo[2,1-i]purinones and ring-enlarged analogues derived from xanthine derivatives have been prepared as adenosine receptor (AR) antagonists. In comparison with xanthines, the tricyclic compounds exhibit increased water solubility due to a basic nitrogen atom, which can be protonated under phys... |
12139453 | New inhibitors of bacterial protein synthesis from a combinatorial library of macrocycles. | A mixture-based combinatorial library of 14-membered macrocycles was synthesized to target ribosomal RNA and uncover a new class of antibacterial agents. High-throughput screening identified a macrocyclic mixture that inhibited cell-free-coupled transcription/translation in Escherichia coli-derived extracts, with an IC... |
12138184 | Multiple regulatory domains of IRF-5 control activation, cellular localization, and induction of chemokines that mediate recruitment of T lymphocytes. | Transcription factors of the interferon regulatory factor (IRF) family have been identified as critical mediators of early inflammatory gene transcription in infected cells. We recently determined that, besides IRF-3 and IRF-7, IRF-5 serves as a direct transducer of virus-mediated signaling. In contrast to that mediate... |
12137760 | Deletional analysis of the rod photoreceptor cell peripherin/RDS carboxy-terminal region. | The C-terminal region of peripherin/rds contains three predicted alpha-helical domains. One of these domains, corresponding to amino acids 311-322, form an amphiphilic alpha-helix previously shown to promote membrane fusion. The present studies were conducted to determine how the additional alpha-helical regions of the... |
12134037 | The block in assembly of modified vaccinia virus Ankara in HeLa cells reveals new insights into vaccinia virus morphogenesis. | It has previously been shown that upon infection of HeLa cells with modified vaccinia virus Ankara (MVA), assembly is blocked at a late stage of infection and immature virions (IVs) accumulate (G. Sutter and B. Moss, Proc. Natl. Acad. Sci. USA 89:10847-10851, 1992). In the present study the morphogenesis of MVA in HeLa... |
12134012 | Genetic and biochemical analyses of receptor and cofactor determinants for T-cell-tropic feline leukemia virus infection. | Entry by retroviruses is mediated through interactions between the viral envelope glycoprotein and the host cell receptor(s). We recently identified two host cell proteins, FeLIX and Pit1, that are necessary for infection by cytopathic, T-cell-tropic feline leukemia viruses (FeLV-T). Pit1 is a classic multiple transmem... |
12133722 | Dendritic polymer macromolecular carriers for drug delivery. | Dendrimers are synthetic, highly branched, mono-disperse macromolecules of nanometer dimensions. Started in the mid-1980s, the research investigations into the synthetic methodology, physical and chemical properties of these macromolecules are increasing exponentially with growing interest in this field. Potential appl... |
11985494 | Mapping the human translation elongation factor eEF1H complex using the yeast two-hybrid system. | In eukaryotes, the eukaryotic translation elongation factor eEF1A responsible for transporting amino-acylated tRNA to the ribosome forms a higher-order complex, eEF1H, with its guanine-nucleotide-exchange factor eEF1B. In metazoans, eEF1B consists of three subunits: eEF1B alpha, eEF1B eta and eEF1B gamma. The first two... |
11972450 | Alteration in the cytosolic triacylglycerol biosynthetic machinery leads to decreased cell growth and triacylglycerol synthesis in oleaginous yeast. | Altered nutrient content (levels of glucose) caused a drastic reduction in cell growth and triacylglycerol (TAG) production in the wild-type (WT) Rhodotorula glutinis. This was due to the decreased level of synthesis of TAG biosynthetic enzymes, reflected by a reduction in enzyme activity. A similar observation was mad... |
11955282 | Support for a three-dimensional structure predicting a Cys-Glu-Lys catalytic triad for Pseudomonas aeruginosa amidase comes from site-directed mutagenesis and mutations altering substrate specificity. | The aliphatic amidase from Pseudomonas aeruginosa belongs to the nitrilase superfamily, and Cys(166) is the nucleophile of the catalytic mechanism. A model of amidase was built by comparative modelling using the crystal structure of the worm nitrilase-fragile histidine triad fusion protein (NitFhit; Protein Data Bank a... |
11939909 | Association of brain gamma-tubulins with alpha beta-tubulin dimers. | gamma-Tubulin is necessary for nucleation and polar orientation of microtubules in vivo. The molecular mechanism of microtubule nucleation by gamma-tubulin and the regulation of this process are not fully understood. Here we show that there are two gamma-tubulin forms in the brain that are present in complexes of vario... |
12127722 | Atherosclerosis: another protein misfolding disease? | The secondary structure and conformation of apo-B 100 in low-density lipoproteins (LDL) are imposed by lipid-protein interactions and dynamics, and affected by the introduction or removal of lipids during the course of lipoprotein metabolism. Following an alteration of the water-lipid interface as a result of, for exam... |
12128056 | Beta-cyclodextrin facilitates cholesterol efflux from larval Manduca sexta fat body and midgut in vitro. | The ability of 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD) and methyl-beta-cyclodextrin (MbetaCD) to promote cholesterol efflux from [3H]cholesterol-labeled larval Manduca sexta fat body and midgut was tested. In fat body, both beta-cyclodextrins induced a two-phase efflux of cholesterol. The first rapid phase depende... |
12125032 | Enantioselective chromatography of alkyl derivatives of 5-ethyl-5-phenyl-2-thiobarbituric acid studied by semiempirical AM1 method. | Complexation of alkyl derivatives of 5-ethyl-5-phenyl-2-thiobarbituric acid (2-thiophenobarbital) enantiomers by beta-cyclodextrin was investigated by the AM1 method. The inclusion complexes of beta-cyclodextrin with neutral and anionic forms of these enantiomers have been modeled and energetically optimized. The chira... |
12124300 | Supramolecular structure in full-length Alzheimer's beta-amyloid fibrils: evidence for a parallel beta-sheet organization from solid-state nuclear magnetic resonance. | We report constraints on the supramolecular structure of amyloid fibrils formed by the 40-residue beta-amyloid peptide associated with Alzheimer's disease (A beta(1-40)) obtained from solid-state nuclear magnetic resonance (NMR) measurements of intermolecular dipole-dipole couplings between (13)C labels at 11 carbon si... |
12124299 | Supramolecular properties of the proline-rich gamma-Zein N-terminal domain. | Zeins are maize storages proteins that accumulate inside large vesicles called protein bodies. gamma-Zein lines the inner face of the protein body membrane, and its N-terminal proline-rich repetitive domain with the sequence (VHLPPP)(8) appears to be necessary for the accumulation of the protein within the organelle. S... |
12124297 | Quaternary structure built from subunits combining NMR and small-angle x-ray scattering data. | A new principle in constructing molecular complexes from the known high-resolution domain structures joining data from NMR and small-angle x-ray scattering (SAXS) measurements is described. Structure of calmodulin in complex with trifluoperazine was built from N- and C-terminal domains oriented based on residual dipola... |
12124294 | Intermolecular interactions, nucleation, and thermodynamics of crystallization of hemoglobin C. | The mutated hemoglobin HbC (beta 6 Glu-->Lys), in the oxygenated (R) liganded state, forms crystals inside red blood cells of patients with CC and SC diseases. Static and dynamic light scattering characterization of the interactions between the R-state (CO) HbC, HbA, and HbS molecules in low-ionic-strength solutions sh... |
12124281 | Structural transitions in short-chain lipid assemblies studied by (31)P-NMR spectroscopy. | The self-assembled supramolecular structures of diacylphosphatidylcholine (diC(n)PC), diacylphosphatidylethanolamine (diC(n)PE), diacylphosphatidyglycerol (diC(n)PG), and diacylphosphatidylserine (diC(n)PS) were investigated by (31)P nuclear magnetic resonance (NMR) spectroscopy as a function of the hydrophobic acyl ch... |
12124268 | Fluid shear regulates the kinetics and molecular mechanisms of activation-dependent platelet binding to colon carcinoma cells. | This study was undertaken to investigate the kinetics and molecular requirements of platelet binding to tumor cells in bulk suspensions subjected to a uniform linear shear field, using a human colon adenocarcinoma cell line (LS174T) as a model. The effects of shear rate (20-1000 s(-1)), shear exposure time (30-300 s), ... |
12121943 | Efficacy of proton pump inhibitor drugs against Plasmodium falciparum in vitro and their probable pharmacophores. | The substituted benzimidazoles omeprazole, lansoprazole, rabeprazole, and pantoprazole were found to have in vitro activity against three different isolates of Plasmodium falciparum: D6 (which is chloroquine and pyrimethamine sensitive), W2 (chloroquine and pyrimethamine resistant), and TM91C235 (multidrug resistant). ... |
12121932 | Safety, pharmacokinetics, and pharmacodynamics of cyclodextrin itraconazole in pediatric patients with oropharyngeal candidiasis. | The safety, pharmacokinetics, and pharmacodynamics of cyclodextrin itraconazole (CD-ITRA) oral suspension were investigated in an open sequential dose escalation study with 26 human immunodeficiency virus (HIV)-infected children and adolescents (5 to 18 years old; mean CD4(+)-cell count, 128/microl) with oropharyngeal ... |
12121931 | Pharmacokinetics and safety of voriconazole following intravenous- to oral-dose escalation regimens. | In this study, the safety, tolerability, and pharmacokinetics of intravenous (i.v.)- to oral-dose regimens of voriconazole were evaluated with a group of 42 healthy men, 41 of whom completed the study. Two cohorts of subjects participated in the study. Cohort 1 (n = 28) took part in two study periods, each consisting o... |
12121907 | Preclinical and toxicology studies of 1263W94, a potent and selective inhibitor of human cytomegalovirus replication. | 1263W94 is a novel benzimidazole compound being developed for treatment of human cytomegalovirus infection. No adverse pharmacological effects were demonstrated in safety pharmacology studies with 1263W94. The minimal-effect dose in a 1-month rat study was 100 mg/kg/day, and the no-effect dose in a 1-month monkey study... |
12117968 | Identification of Escherichia coli outer membrane protein A receptor on human brain microvascular endothelial cells. | Neonatal Escherichia coli meningitis continues to be a diagnostic and treatment challenge despite the availability of active antibiotics. Our earlier studies have shown that outer membrane protein A (OmpA) is one of the major factors responsible for Escherichia coli traversal across the blood-brain barrier that constit... |
12117922 | Eighty-kilodalton N-terminal moiety of Bordetella pertussis filamentous hemagglutinin: adherence, immunogenicity, and protective role. | Bordetella pertussis, the etiological agent of whooping cough, produces a number of factors, such as toxins and adhesins, that are required for full expression of virulence. Filamentous hemagglutinin (FHA) is the major adhesin of B. pertussis. It is a protein of approximately 220 kDa, found both associated at the bacte... |
12117919 | Plasma membrane cholesterol modulates cellular vacuolation induced by the Helicobacter pylori vacuolating cytotoxin. | The Helicobacter pylori vacuolating cytotoxin (VacA) induces the degenerative vacuolation of mammalian cells both in vitro and in vivo. Here, we demonstrate that plasma membrane cholesterol is essential for vacuolation of mammalian cells by VacA. Vacuole biogenesis in multiple cell lines was completely blocked when cho... |
12117911 | Proteasomal degradation of cytotoxic necrotizing factor 1-activated rac. | The cytotoxic necrotizing factor 1 (CNF1) from Escherichia coli has been shown to activate members of the Rho family by deamidation of glutamine 63. This amino acid is essential for hydrolysis of GTP, and any substitution results in a constitutively active Rho. Activation of Rho induces the formation of stress fibers, ... |
12115815 | Ultrasound-compacted indomethacin/polyvinylpyrrolidone systems: effect of compaction process on particle morphology and dissolution behavior. | Indomethacin (IMC)/polyvinylpyrrolidone systems were prepared under different technological conditions, using co-evaporation, kneading, traditional, and ultrasound (US) compaction. The materials thus obtained were milled and sieved and the powders were analyzed by using scanning electron microscopy to evaluate the morp... |
12115808 | Solubilization of hydrophobic drugs in octanoyl-6-O-ascorbic acid micellar dispersions. | Alkanoyl-6-O-ascorbic acid esters are easily obtained from vitamin C, and produce self-assembled aggregates in water solutions, with an inner hydrophobic pool surrounded by an external hydrophilic shell. Compared to ascorbic acid, their solubility in oils and fats is greatly enhanced, while the peculiar antioxidant act... |
12115409 | Anchorage of cyclodextrin glucanotransferase on the outer membrane of Escherichia coli. | The gene encoding cyclodextrin glucanotransferase (CGTase) was successfully cloned from B. macerans by PCR. A recombinant plasmid pCS005 with a gene encoding the Lpp-OmpA-CGTase trifusion protein was constructed and transformed into E. coli for the surface display of CGTase. Results of immunoblotting analysis and prote... |
12112677 | Monte Carlo simulations of the peptide recognition at the consensus binding site of the constant fragment of human immunoglobulin G: the energy landscape analysis of a hot spot at the intermolecular interface. | Monte Carlo simulations of molecular recognition at the consensus binding site of the constant fragment (Fc) of human immunoglobulin G (Ig) protein have been performed to analyze structural and thermodynamic aspects of binding for the 13-residue cyclic peptide DCAWHLGELVWCT. The energy landscape analysis of a hot spot ... |
12110397 | Determination of adrenergic agonists from extracts and herbal products of Citrus aurantium L. var. amara by LC. | The purpose of this study was to set up a HPLC method to separate adrenergic amines (dl-octopamine, dl-synephrine and tyramine) and to determine their content in fruits, extracts and herbal products of Citrus aurantium L. var. amara. A rapid method for the quantitative analysis of these amines is described, based on th... |
12110386 | Characterization of physicochemical properties of naproxen systems with amorphous beta-cyclodextrin-epichlorohydrin polymers. | Ground mixtures of naproxen with amorphous beta-cyclodextrin-epichlorohydrin soluble (betaCd-EPS) or insoluble cross-linked (betaCd-EPI) polymers were investigated for both solid phase characterization (Differential Scanning Calorimetry, powder X-ray Diffractometry) and dissolution properties (dispersed amount method).... |
12110385 | Study of flavonoids/beta-cyclodextrins inclusion complexes by NMR, FT-IR, DSC, X-ray investigation. | Flavonoids are natural substances with a lot of biological activities, including the antioxidant one. Their use in pharmaceutical field is, however, limited by their aqueous insolubility. As the formation of the inclusion complexes can improve their solubility in water, the flavonoids hesperetin, hesperidin, naringenin... |
12110384 | Chiral separation of methoxamine and lobeline in capillary zone electrophoresis using ethylbenzene-deactivated fused-silica capillary columns and cyclodextrins as buffer additives. | The complete chiral separation of methoxamine and lobeline was achieved by capillary zone electrophoresis on an ethylbenzene-deactivated fused-silica capillary column and with cyclodextrins (CDs) as buffer additives. Among the CDs investigated in this study, i.e. alpha-CD, beta-CD, dimethyl-beta-CD, hydroxypropyl-beta-... |
12110382 | Determination of losartan and hydrochlorothiazide in tablets by CE and CEC. | Capillary Electrophoresis (CE) and Capillary Electrochromatography (CEC) have been used to determine losartan and hydrochlorothiazide. The CE separation was carried out in an uncoated capillary filled with a 100 mM sodium borate pH 9 solution containing trimethyl-beta-cyclodextrins. CEC was performed using a capillary ... |
12107138 | Cooperativity in signal transfer through the Uhp system of Escherichia coli. | The UhpABC regulatory system in enterobacteria controls the expression of the hexose phosphate transporter UhpT. Signaling is initiated through sensing of extracellular glucose 6-phosphate by membrane-bound UhpC, which in turn modulates the histidine-protein kinase UhpB. Together with the cytoplasmic response regulator... |
12107137 | Antigen 43-mediated autotransporter display, a versatile bacterial cell surface presentation system. | Antigen 43 (Ag43), a self-recognizing outer membrane protein of Escherichia coli, has been converted into an efficient and versatile tool for surface display of foreign protein segments. Ag43 is an autotransporter protein characterized by the feature that all information required for transport to the outer membrane and... |
12103432 | Evidence of dual sites of action of dendrimers: SPL-2999 inhibits both virus entry and late stages of herpes simplex virus replication. | Dendrimers are macromolecules with broad-spectrum antiviral activity and minimal toxicity effective in animal models in preventing transmission of herpes simplex virus (HSV) infection. In order to further understand the mechanism of action, and toxicity profiles of the dendrimer SPL-2999 against HSV, we investigated in... |
12099278 | Interactions between dendrimer biocides and bacterial membranes. | Dendrimer biocides have been shown to be more potent than their small molecule counterparts. In this study, several techniques were utilized to investigate the interactions between quaternary ammonium functionalized poly(propylene imine) dendrimers and bacterial membranes. Both Gram-positive and Gram-negative bacteria ... |
12097564 | Novel monoclonal antibody directed at the receptor binding site on the avian sarcoma and leukosis virus Env complex. | We report here on the generation of a mouse monoclonal antibody directed against Rous sarcoma virus (RSV) subgroup A Env that will be useful in functional and structural analysis of RSV Env, as well as in approaches employing the RCAS/Tva system for gene targeting. BALB/c mice were primed and given boosters twice with ... |
12057636 | Computer-aided simulation of a dendrimer with a protoporphyrinic core as potential, novel hemoprotein mimic. | In this work, we have inserted the ion-heme group characterizing human blood in a class of synthetic, dendrimeric macromolecules, to evaluate a series of structural and physico-chemical properties related to the possible biological activity of these polymers. To this purpose, we have performed a complete series of inve... |
12151400 | ATP-dependent hexameric assembly of the heat shock protein Hsp101 involves multiple interaction domains and a functional C-proximal nucleotide-binding domain. | Members of the Hsp100 family of heat stress proteins are present in species throughout the bacterial, plant, and fungal kingdoms. Most Hsp100 proteins are composed of five domains that include two nucleotide-binding domains required for their ATP-dependent oligomerization. Mutations within the first but not the second ... |
12154314 | A pseudo-quadruple hydrogen-bonding motif consisting of six N-H...O hydrogen bonds in trimethoprim formate. | The title compound, trimethoprim (TMP) formate [systematic name: 2,4-diamino-5-(3,4,5-trimethoxybenzyl)pyrimidin-1-ium formate], C(14)H(19)N(4)O(3)(+).CHO(2)(-), reveals a pseudo-quadruple hydrogen-bonding motif consisting of six N-H.O hydrogen bonds involving two unpaired TMP cations and two formate anions which are s... |
12149466 | Adipose tissue mass can be regulated through the vasculature. | Tumor growth is angiogenesis dependent. We hypothesized that nonneoplastic tissue growth also depends on neovascularization. We chose adipose tissue as an experimental system because of its remodeling capacity. Mice from different obesity models received anti-angiogenic agents. Treatment resulted in dose-dependent, rev... |
12149440 | The molecular structure of spider dragline silk: folding and orientation of the protein backbone. | The design principles of spider dragline silk, nature's high-performance fiber, are still largely unknown, in particular for the noncrystalline glycine-rich domains, which form the bulk of the material. Here we apply two-dimensional solid-state NMR to determine the distribution of the backbone torsion angles (phi,psi) ... |
12145328 | The multidrug transporter, P-glycoprotein, actively mediates cholesterol redistribution in the cell membrane. | P-glycoprotein (P-gp) is a plasma membrane ATP-binding cassette transporter, responsible for multidrug resistance in tumor cells. P-gp catalyzes the ATP hydrolysis-dependent efflux of numerous amphiphilic compounds of unrelated chemical structures. In the absence of any identified substrate, P-gp exhibits an apparently... |
12136134 | In vivo quantification of localized neuronal activation and inhibition in the rat brain using a dedicated high temporal-resolution beta +-sensitive microprobe. | Understanding brain disorders, the neural processes implicated in cognitive functions and their alterations in neurodegenerative pathologies, or testing new therapies for these diseases would benefit greatly from combined use of an increasing number of rodent models and neuroimaging methods specifically adapted to the ... |
12134166 | Magnetic relaxation switches capable of sensing molecular interactions. | Highly sensitive, efficient, and high-throughput biosensors are required for genomic and proteomic data acquisition in complex biological samples and potentially for in vivo applications. To facilitate these studies, we have developed biocompatible magnetic nanosensors that act as magnetic relaxation switches (MRS) to ... |
12135985 | Role of KIFC3 motor protein in Golgi positioning and integration. | KIFC3, a microtubule (MT) minus end-directed kinesin superfamily protein, is expressed abundantly and is associated with the Golgi apparatus in adrenocortical cells. We report here that disruption of the kifC3 gene induced fragmentation of the Golgi apparatus when cholesterol was depleted. Analysis of the reassembly pr... |
12154311 | Hydrogen bonding in 2-(hydroxymethyl)-1,3-propanediol and N,N'-bis[2-hydroxy-1,1-bis(hydroxymethyl)ethyl]malonamide. | The molecule of 2-(hydroxymethyl)-1,3-propanediol, C(4)H(10)O(3), lies across a mirror plane in space group P2(1)/m, with disorder of both terminal hydroxyl H atoms. The molecules are linked by three O-H...O hydrogen bonds which combine to form sheets; in each O-H...O bond, the H atom resonates between the two O atoms.... |
12154307 | 2-Iodo-N-(3-nitrobenzyl)aniline and 3-iodo-N-(3-nitrobenzyl)aniline exhibit entirely different patterns of supramolecular aggregation. | In 2-iodo-N-(3-nitrobenzyl)aniline, C(13)H(11)IN(2)O(2), the molecules are linked into a three-dimensional structure by a combination of C-H...O hydrogen bonds, iodo-nitro interactions and aromatic pi-pi-stacking interactions, but N-H...O and C-H...pi(arene) hydrogen bonds are absent. In the isomeric 3-iodo-N-(3-nitrob... |
12154306 | 2-Nitrophenyl 4-nitrophenyl disulfide. | The structure of the title compound, C(12)H(8)N(2)O(4)S(2), contains no direction-specific intermolecular interactions, i.e. no C-H...O hydrogen bonds, no aromatic pi-pi-stacking interactions and no C-H...pi(arene) interactions. This behaviour is compared with the three known symmetrical isomers of bis(nitrophenyl) dis... |
12124399 | A human embryonic hemoglobin inhibits Hb S polymerization in vitro and restores a normal phenotype to mouse models of sickle cell disease. | The principle that developmentally silenced globin genes can be reactivated in adults with defects in beta-globin gene expression has been well established both in vitro and in vivo. In practice, levels of developmental stage-discordant fetal gamma globin that can be achieved by using currently approved therapies are g... |
12226716 | Enzymatic production of cyclodextrins. | Cyclodextrins (CD) are enzymatically modified starches with a wide range of applications in food, pharmaceutical and chemical industries, agriculture and environmental engineering. They are produced from starch via enzymatic conversion using cyclodextrin glycosyl transferases (CGTases) and partly alpha-amylases. Due to... |
12121984 | Association of Helicobacter pylori vacuolating toxin (VacA) with lipid rafts. | A variety of extracellular ligands and pathogens interact with raft domains in the plasma membrane of eukaryotic cells. In this study, we examined the role of lipid rafts and raft-associated glycosylphosphatidylinositol (GPI)-anchored proteins in the process by which Helicobacter pylori vacuolating toxin (VacA) intoxic... |
12119400 | Structure of decay-accelerating factor bound to echovirus 7: a virus-receptor complex. | Echoviruses are enteroviruses that belong to Picornaviridae. Many echoviruses use decay-accelerating factor (DAF) as their cellular receptor. DAF is a glycosylphosphatidyl inositol-anchored complement regulatory protein found on most cell surfaces. It functions to protect cells from complement attack. The cryo-electron... |
12118241 | Monitoring post-translational modification of proteins with allosteric ribozymes. | An allosteric hammerhead ribozyme activated specifically by the unphosphorylated form of the protein kinase ERK2 was created through a rational design strategy that relies on molecular recognition of ERK2 to decrease the formation of an alternate, inactive ribozyme conformer. Neither closely related mitogen-activated p... |
12119419 | Self-assembling biomaterials: liquid crystal phases of cholesteryl oligo(L-lactic acid) and their interactions with cells. | We report here on the synthesis and characterization of a series of self-assembling biomaterials with molecular features designed to interact with cells and scaffolds for tissue regeneration. The molecules of these materials contain cholesteryl moieties, which have universal affinity for cell membranes, and short chain... |
12119416 | Crystal structure of monomeric human beta-2-microglobulin reveals clues to its amyloidogenic properties. | Dissociation of human beta-2-microglobulin (beta(2)m) from the heavy chain of the class I HLA complex is a critical first step in the formation of amyloid fibrils from this protein. As a consequence of renal failure, the concentration of circulating monomeric beta(2)m increases, ultimately leading to deposition of the ... |
12119415 | Molecular recognition of oxygen by protein mimics: dynamics on the femtosecond to microsecond time scale. | Molecular recognition by biological macromolecules involves many elementary steps, usually convoluted by diffusion processes. Here we report studies of the dynamics, from the femtosecond to the microsecond time scale, of the different elementary processes involved in the bimolecular recognition of a protein mimic, coba... |
12119412 | Multiple label-free biodetection and quantitative DNA-binding assays on a nanomechanical cantilever array. | We report a microarray of cantilevers to detect multiple unlabeled biomolecules simultaneously at nanomolar concentrations within minutes. Ligand-receptor binding interactions such as DNA hybridization or protein recognition occurring on microfabricated silicon cantilevers generate nanomechanical bending, which is dete... |
12119393 | Self-assembling peptide hydrogel fosters chondrocyte extracellular matrix production and cell division: implications for cartilage tissue repair. | Emerging medical technologies for effective and lasting repair of articular cartilage include delivery of cells or cell-seeded scaffolds to a defect site to initiate de novo tissue regeneration. Biocompatible scaffolds assist in providing a template for cell distribution and extracellular matrix (ECM) accumulation in a... |
12117999 | Hsp90 interactions and acylation target the G protein Galpha 12 but not Galpha 13 to lipid rafts. | The heterotrimeric G proteins, G(12) and G(13), are closely related in their sequences, signaling partners, and cellular effects such as oncogenic transformation and cytoskeletal reorganization. Yet G(12) and G(13) can act through different pathways, bind different proteins, and show opposing actions on some effectors.... |
12154303 | (1SR,2RS,5RS,6SR,8RS)-7,7-Dimethyltricyclo[6.2.1.0(1,6)]undecane-2,5,6-triol: a supramolecular framework built from O-H...O hydrogen bonds. | In the title compound, C(13)H(22)O(3), the asymmetric unit has two independent molecules linked by a strong O-H...O hydrogen bond. The cyclohexane ring is trans fused to the cyclopentane ring bridged through an ethyl moiety. The hydroxyl groups act as donors as well as acceptors, resulting in an extensive two-dimension... |
12154300 | 2,6-Diiodo-4-nitrophenol, 2,6-diiodo-4-nitrophenyl acetate and 2,6-diiodo-4-nitroanisole: interplay of hydrogen bonds, iodo-nitro interactions and aromatic pi-pi-stacking interactions to give supramolecular structures in one, two and three dimensions. | In 2,6-diiodo-4-nitrophenol, C(6)H(3)I(2)NO(3), the molecules are linked, by an O-H...O hydrogen bond and two iodo-nitro interactions, into sheets, which are further linked into a three-dimensional framework by aromatic pi-pi-stacking interactions. The molecules of 2,6-diiodo-4-nitrophenyl acetate, C(8)H(5)I(2)NO(4), l... |
12185576 | Polymerized crystalline colloidal array chemical-sensing materials for detection of lead in body fluids. | We have developed intelligent polymerized crystalline colloidal array (IPCCA) chemical-sensing materials for detection of Pb(2+) in high ionic-strength environments such as body fluids with a detection limit of <500 nmol L(-1) Pb(2+) (100 ppb). This IPCCA lead sensor consists of a mesoscopically periodic array of collo... |
12105189 | A cryptic fragment from fibronectin's III1 module localizes to lipid rafts and stimulates cell growth and contractility. | The interaction of cells with the extracellular matrix (ECM) form of fibronectin (FN) triggers changes in growth, migration, and cytoskeletal organization that differ from those generated by soluble FN. As cells deposit and remodel their FN matrix, the exposure of new epitopes may serve to initiate responses unique to ... |
12097647 | Cell surface expression and secretion of heparanase markedly promote tumor angiogenesis and metastasis. | The present study emphasizes the importance of cell surface expression and secretion of heparanase (endo-beta-D-glucuronidase) in tumor angiogenesis and metastasis. For this purpose, nonmetastatic Eb mouse lymphoma cells were transfected with the predominantly intracellular human heparanase or with a readily secreted c... |
12097640 | Protein-solvent preferential interactions, protein hydration, and the modulation of biochemical reactions by solvent components. | Solvent additives (cosolvents, osmolytes) modulate biochemical reactions if, during the course of the reaction, there is a change in preferential interactions of solvent components with the reacting system. Preferential interactions can be expressed in terms of preferential binding of the cosolvent or its preferential ... |
21432289 | Mechanism of cytotoxicity of paraquat. | Acute paraquat poisoning seems to be very complex because many possible mechanisms of paraquat cytotoxicity have been reported. Some may not be the cause of paraquat poisoning but the result or an accompanying phenomenon of paraquat action. The mechanism critical for cell damage is still unknown. Paraquat poisoning is ... |
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