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PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Groups of six mice were then treated with either 20mg/kg alisertib, 30mg/kg Aurkin A, 20mg/kg alisertib + 30mg/kg Aurkin A combination, or a vehicle control (DMSO volume match).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Mice were given the corresponding treatment once a day for five days a week.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
After two weeks, treatment was then withheld for a week, followed by another five-day-a-week treatment cycle.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
One mouse in the combination group died fifteen days into the treatment with no additional mortality events seen in any other mouse groups.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Mouse groups were sacrificed on day 24 as alisertib and control groups were approaching the approved protocol's max tumor size of 2cm.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
A statistically significant difference was found between the combination group and the control (p=0.0153), alisertib (p=0.027), and Aurkin A (p=0.0323) groups.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Mouse tumors were then harvested, formalin-fixed, and hematoxylin and eosin stained.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Cells were then classified as polyploid or normalploid based nucleus to cell area ratio, using the QuPath Bioimaging Analysis software (Fig. 7a and b).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Ploidy analysis from the vehicle control 84.3% normalploid and 15.7% polyploid respectively (Fig. 7c).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Aurkin A treatment showed 83.8% normalploid and 16.2% polyploid cells respectively.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
The alisertib treated group showed a significant increase in polyploidy to 43.6% and decrease in normaloid cells to 56.7%.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
In contrast, Aurkin A plus alisertib reduced polyploidy to levels seen in the control to 16.1% with 83.9% normalploid cells.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Fig. 7Alisertib Induced Polyploidy is Significantly Disrupted by Aurkin A in A VAL Mouse Xenograft Model.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Alisertib induced polyploidy is significantly disrupted by Aurkin A in a VAL mouse xenograft model.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
SCID mice were injected with 1 × 106 VAL cells in sterile saline subcutaneously in the left flank.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Mice were pair matched based on tumor volume three weeks post injection and grouped into an alisertib 20mg/kg, Aurkin A 30mg/kg, Alisertib 20mg/kg + Aurkin A 30mg/kg combination, and vehicle control (DMSO volume match) groups.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Mice were given the corresponding treatment once a day for five days a week.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Treatment was then withheld for two weeks followed by another five-day-a-week treatment cycle.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
One mouse in the combination group died 15 days after the start of treatment.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Tumor volume was normalized to the volume at the start of treatment and graphed.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
There was a statistically significant difference in tumor volume between the combination group and the control (p=0.0153), alisertib (p=0.027), and Aurkin A (p=0.0323) groups (A).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Tumors dissected and fixed in formalin and paraffin embedded.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Slides were H&E stained and QuPath Bioimaging Analysis software performed for nucleus to cell ratio to identify polyploidy cells (B).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
depicts H&E stain from a vehicle control treated mouse.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
The ploidy classification performed by QuPath highlights normalploid cells in green and polyploid cells in blue (C).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Three different fields of at least 10,000 cells were counted for each condition (D).Fig 7 Alisertib Induced Polyploidy is Significantly Disrupted by Aurkin A in A VAL Mouse Xenograft Model.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Alisertib induced polyploidy is significantly disrupted by Aurkin A in a VAL mouse xenograft model.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
SCID mice were injected with 1 × 106 VAL cells in sterile saline subcutaneously in the left flank.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Mice were pair matched based on tumor volume three weeks post injection and grouped into an alisertib 20mg/kg, Aurkin A 30mg/kg, Alisertib 20mg/kg + Aurkin A 30mg/kg combination, and vehicle control (DMSO volume match) groups.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Mice were given the corresponding treatment once a day for five days a week.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Treatment was then withheld for two weeks followed by another five-day-a-week treatment cycle.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
One mouse in the combination group died 15 days after the start of treatment.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Tumor volume was normalized to the volume at the start of treatment and graphed.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
There was a statistically significant difference in tumor volume between the combination group and the control (p=0.0153), alisertib (p=0.027), and Aurkin A (p=0.0323) groups (A).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Tumors dissected and fixed in formalin and paraffin embedded.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Slides were H&E stained and QuPath Bioimaging Analysis software performed for nucleus to cell ratio to identify polyploidy cells (B).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
depicts H&E stain from a vehicle control treated mouse.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
The ploidy classification performed by QuPath highlights normalploid cells in green and polyploid cells in blue (C).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Three different fields of at least 10,000 cells were counted for each condition (D).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Alisertib is an ATP site inhibitor of AK-A, a key regulatory mitotic kinase.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
We characterize cell cycle disruption and resulting polyploidy from alisertib treatment in DLBCL U2932 and VAL cell lines.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Increasing concentrations of alisertib up to 1µM (clinically achieved) displayed increased 4n, 8n, and 16n polyploid cells along with decreased G1 cell populations.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Cells treated with alisertib have a drastically altered morphology, significantly larger and amorphic.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Alisertib treatment of FUCCI U2932 cells shows that one third of all treated cells can generate polyploidy via endomitosis, increasing longevity and resistance to apoptosis.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Additionally, alisertib treatment induces an aggressive growth phenotype, as they can undergo G1 cell cycle slippage, thus shortening the overall cell cycle.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
The VAL mouse xenograft model further evidences this accelerated growth phenotype and longevity of polyploid cells, as alisertib treated tumors had a significantly higher growth rate when compared to the DMSO control treatment.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Aurkin A, a small molecule inhibitor, prevents allosteric binding of TPX2 to the N-terminal kinase domain of AK-A and sensitizes U2932 cells to alisertib.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
This is evidenced as there was a decrease in alisertib IC50 from 983nM to 34nM with the addition of 100µM Aurkin A. MDA-MB-231, Hela, Mia PaCa-2, U-2 OS, Granta-519 cell lines also saw a significant drop in IC50 with the addition of 100µM Aurkin A. Calculated combination indexes show that the combination of alisertib and Aurkin A is synergistic.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
This provides evidence that lower concentrations of alisertib can be used with Aurkin A combination to kill a cell population.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
The addition of Aurkin A to alisertib significantly increased the level of apoptosis in U2932 cells, as 500nM alisertib alone had a viable cell population of 67% which declined to 12% with the addition of 100µM Aurkin A. The combination of Aurkin A plus alisertib inhibits cell cycle slippage and endomitotic activity of alisertib resulting in decreased polyploidy and increased apoptosis.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
An in vivo VAL xenograft mouse model confirmed these results as there was a significant reduction in tumor growth between the combination and other treatment groups.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Additionally, significantly less polyploidy was observed between alisertib treatment (43.6%) and in combination alisertib plus Aurkin A treatment (16.1%).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Interestingly, results from the MTS assays suggest synergy from the combination of alisertib and Aurkin A is not isolated to just DLBCL cell lines.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
However, further testing is required to validate this hypothesis.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
While the mechanism by which alisertib and Aurkin A synergy yet to be fully identified, we hypothesize that the dual inhibition of AK-A by alisertib and Aurkin A results in cell cycle arrest in late G2 or early M, resulting in eventual cell death.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Results from the FUCCI experiments strengthen this hypothesis as approximately 90% of cells treated with the combination therapy were unable to progress past G2/M resulting in cell cycle arrest and eventual cell death.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
However, 10% combination cells failed to progress to through G1, leading to cell cycle arrest and cell death.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
This phenotype could still be explained by the AK-A dual inhibition hypothesis, as it is possible that cell undergoing mitosis at the time of treatment may have experienced significant DNA damage, or chromosomal mis-segregation due to AK-A/AK-B inhibition.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
This DNA damage could prevent progression through the S phase DNA damage checkpoint and lead to cell death.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
A phase II clinical trial of alisertib conducted in 48 patients with aggressive B- and T- cell NHL described the safety, toxicity profile and maximum tolerated dose (MTD) .
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Pharmacokinetic analysis of alisertib showed a mean effective dose to be 2.375µM, however, the MTD was established at 1.504µM .
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
The sensitization of alisertib with Aurkin A in complete AK-A inhibition is of high clinical importance as the alisertib dose can be reduced by 3-fold not only to prevent polyploidy, enhance efficacy but significantly reduce toxicity to normal tissue.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Apoptosis data in U2932 cells shows a viable cell population of 39% after five days of 5µM alisertib treatment, which declined to 22% after four days without treatment.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
At 500nM alisertib a five-day viable population of 67% improved to 82% after four days without treatment.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
However, addition of 100µM Aurkin A to 500nM alisertib produced a viable population of 12% which increased to 19% post treatment.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
This change in viable populations strongly suggests that Aurkin A significantly sensitizes U2932 and VAL cells to alisertib, more than 10-fold of alisertib alone.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
In addition, it potentiates killing of polyploid cells, which could help limit cancer recurrence.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
This Aurkin A effect warrants further investigation in other cancer cell types and with chemotherapeutic agents that induced drug-resistant polyploidy.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
This research was supported by R21ES035997 from NIEHS to E. Dray.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
The Mays Cancer Center (MCC) is supported by a grant from the National Cancer Institute (P30CA054174; Sung, P.).
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
The Flow Cytometry Shared Resource at UT Health San Antonio is supported by grants from the Cancer Prevention and Research Institute of Texas (RP210126; Berton, M.T.) and from the National Institutes of Health (S10OD030432; Berton, M.T.), and support from the MCC and the Office of the Vice President for Research at UT Health San Antonio.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Patrick J. Conway: Writing – original draft, Validation, Methodology, Investigation, Formal analysis, Data curation.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Bárbara De La Peña Avalos: Investigation, Data curation.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Jonathan Dao: Investigation, Data curation.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Sebastian Montagnino: Investigation, Data curation.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Dmytro Kovalskyy: Visualization, Software.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Eloise Dray: Writing – review & editing, Validation, Supervision, Resources, Project administration, Methodology, Conceptualization.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
Daruka Mahadevan: Writing – review & editing, Validation, Supervision, Resources, Project administration, Methodology, Conceptualization.
PMC11225860
Aurkin-A, a TPX2-aurora a small molecule inhibitor disrupts Alisertib-induced polyploidy in aggressive diffuse large B cell lymphoma
The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Chemotaxis is an essential physiological process, often harnessed by tumors for metastasis.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
CXCR4, its ligand CXCL12 and the atypical receptor ACKR3 are overexpressed in many human cancers.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Interfering with this axis by ACKR3 deletion impairs lymphoma cell migration towards CXCL12.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Here, we propose a model of how ACKR3 controls the migration of the diffused large B-cell lymphoma VAL cells in vitro and in vivo in response to CXCL12.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
VAL cells expressing full-length ACKR3, but not a truncated version missing the C-terminus, can support the migration of VAL cells lacking ACKR3 (VAL-ko) when allowed to migrate together.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
This migration of VAL-ko cells is pertussis toxin-sensitive suggesting the involvement of a Gi-protein coupled receptor.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
RNAseq analysis indicate the expression of chemotaxis-mediating LTB4 receptors in VAL cells.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
We found that LTB4 acts synergistically with CXCL12 in stimulating the migration of VAL cells.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Pharmacologic or genetic inhibition of BLT1R markedly reduces chemotaxis towards CXCL12 suggesting that LTB4 enhances in a contact-independent manner the migration of lymphoma cells.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
The results unveil a novel mechanism of cell-to-cell-induced migration of lymphoma.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Cell migration is a widely conserved biological process, but the involved intracellular pathways are poorly understood.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Directional migration or chemotaxis is orchestrated by distinct cell surface receptors, which guide cells along gradients of increasing concentrations of attractants (1).
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Chemokines, which constitute the largest family of chemoattractants, share a basic isoelectric point that allows them to be presented on cell surfaces and extracellular matrices (2, 3).
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
They induce chemotaxis by binding to cognate G-protein-coupled receptors (GPCRs), which upon ligand binding activate via pertussis toxin-sensitive G proteins downstream pathways leading to cell migration (4, 5).
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
In addition to conventional G-protein coupled chemokine receptors, chemokines bind to seven-transmembrane domain receptors, which do not activate G-proteins, called atypical chemokine receptors (ACKR) (3–5).
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
ACKR3 acts mainly as a decoy with high affinity for the chemokine CXCL12 and with lower affinity for CXCL11, which are also ligands for the conventional receptors CXCR4 and CXCR3, respectively (6, 7).
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
The physiological importance of the CXCL12/ACKR3/CXCR4 axis is underlined by the fact that absence of either component causes perinatal death in mice severely disrupting central nervous system and heart development (8–11).
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Chemotaxis is governed by a chemokine-producing source, often constituted by stromal cells, and a juxtaposed sink that removes chemokines, either cells that express ACKRs or other mechanisms of degradation.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Removal of chemoattractants is essential to maintain gradients and to avoid blurring of the source.
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Chemokine gradients are established over a relatively short distance of about 100 to 150 µm (12).
PMC9878562
ACKR3 promotes CXCL12/CXCR4-mediated cell-to-cell-induced lymphoma migration through LTB4 production
Therefore, chemotaxis is not involved in long distance cell displacements as observed in passive blood-flow mediated cell movement (13).