Oncology and Immunology The β2-adrenergic receptor associates with CXCR4 multimers in human cancer cells PIE-FCCS can resolve membrane protein density, diffusion, and multimerization state in live cells at into multimeric complexes larger than dimers in MDA-MB-231 human breast cancer cells and in HCC4006 human lung cancer cells. than in COS-7 and CHO cells and in a ligand-dependent manner.

in Oncology and Immunology Autocrine proteinase-activated receptor signaling in PC3 prostate cancer cells PARs are highly expressed in many cancer cells, including prostate cancer (PCa), and regulate various In this study, we examined the androgen-independent human prostatic cancer cell line PC3 and find the Using genetically encoded PAR cleavage biosensors, we showed that PC3 cells secrete proteolytic enzymes of PAR1 promotes PC3 cell migration and suppresses cell proliferation, whereas PAR2 deficiency showed

Oncology and Immunology Comparative analysis of the occupancy of Histone H3 Lysine 4 methylation in the cells 28, 2023 Abstract "In this current study, we have compared our H3K4me3 Chip-Sequencing data in PC3 cells in response to 6h and 24h TGFβ stimulation with the IFNγ stimulated/unstimulated HeLa S3 cells Since modification changes in response to TGFβ and IFNγ and compare them to explore the genes common to both as well Functional enrichment analysis in the TGFβ and IFNγ dataset revealed association of genes with different biological

Immunology Systems Pharmacodynamic Model of Combination Gemcitabine and Trabectedin in Pancreatic Cancer Cells Part II: Cell Cycle, DNA Damage Response, and Apoptosis Pathways Published date October 31, 2023 Abstract , we reported the synergistic cytotoxic effects of gemcitabine and trabectedin on pancreatic cancer cells Here we describe drug effects on pathways associated with cell cycle, DNA damage response (DDR), and The SPD model was subsequently incorporated into our previously-established cell cycle model, forming

< GPCR News < GPCRs in Oncology and Immunology GPR4 in the pH-dependent migration of melanoma cells in pH-gradient) is a well-known driver of tumor progression and metastasis. In this study, we investigated the pH-dependent migration of GPR4 wildtype/overexpressing SK-Mel-28 cells Migration of GPR4 overexpressing SK-Mel-28 cells was enhanced in a range of pH 6.5 - pH 7.5 as compared Results indicate that GPR4 is involved in the migration of melanoma cells, especially in the tumor periphery

in Oncology and Immunology LPA1-mediated inhibition of CXCR4 attenuates CXCL12-induced signaling and cell Results: We observed that CXCR4 forms heteromers with LPA1 in recombinant HEK293A cells and the human breast cancer cell line MDA-MB-231. MDA-MB-231 cells but not in LPA1-deficient cells. have been evidenced across various cell lines.

< GPCR News < GPCRs in Oncology and Immunology Activation of orphan receptor GPR132 induces cell differentiation Here, we showed that genetic activation of the orphan GPCR GPR132 significantly induced cell differentiation Notably, GPR132 activation by 8GL promoted differentiation and reduced colony formation in human AML cell We further showed that the combination of 8GL and an mTOR inhibitor synergistically elicited AML cell impaired tumor growth and extended mouse survival in an AML xenograft model accompanied by enhanced cell

GPCR News < GPCRs in Oncology and Immunology G protein coupled receptor transcripts in human immune cells We have used the method to profile GPCR transcripts in white blood cells (WBCs)-B, CD4, CD8, NK, and dendritic cells; monocytes, and macrophage-like monocytes treated with granulocyte-macrophage colony-stimulating factor-as well as platelets. On average, the white cells studied expressed 160 receptor mRNAs (range, 123-206).

News < GPCRs in Oncology and Immunology The orphan G protein-coupled receptor 141 expressed in myeloid cells High GPR141 messenger RNA levels were expressed in myeloid-lineage cells, including neutrophils (CD11b Gpr141 -/- mice, which we independently generated, displayed almost no abnormalities in myeloid cell myelin oligodendrocyte glycoprotein 35-55-specific T cells. , experimental autoimmune encephalomyelitis , monocytes , myeloid cells .

< GPCR News < GPCRs in Oncology and Immunology The EBI2 receptor is coexpressed with CCR5 in CD4+ T cells Methods: We identified GPCRs expressed in primary CD4+CCR5+ T cells by multi-RT-qPCR. Cell lines expressing EBI2 were established by transduction with HIV vectors. The amount of HIV reverse transcripts was similar in cells expressing or not EBI2. Conclusions: EBI2 expression in CD4+CCR5+ cells boosts HIV-1 R5 productive infection.

in Oncology and Immunology Vasoactive intestinal peptide receptor 2 signaling promotes breast cancer cell cell lines, promoted cell proliferation. proliferation in VIPR2-overexpressing MCF-7 and MDA-MB-231 cells. was greater than that in control cells, suggesting the increased PKA activity. at the same level as observed in EGFP-expressing cells treated with U0126.

< GPCR News < GPCRs in Oncology and Immunology NPFF stimulates human ovarian cancer cell invasion by The TaqMan probe-based RT-qPCR showed that NPFF and NPFFR2 were expressed in three human EOC cells, CaOV3 In comparison, NPFF and NPFFR2 expression levels were higher in SKOV3 cells than in CaOV3 or OVCAR3 cells Treatment of SKOV3 cells with NPFF did not affect cell viability and proliferation but stimulated cell This study provides evidence that NPFF stimulates EOC cell invasion by upregulating MMP-9 expression

Immunology The pyruvate-GPR31 axis promotes transepithelial dendrite formation in human intestinal dendritic cells intestinal lumen is rich in gut microbial metabolites that serve as signaling molecules for gut immune cells by the gut bacterial metabolite pyruvate, is specifically expressed on type 1 conventional dendritic cells Using human induced pluripotent stem cell-derived cDC1s and a monolayer human gut organoid coculture Kumanogoh, Kiyoshi Takeda Tags G protein-coupled receptors , GPR31 , antigen recognition , dendritic cell

< GPCR News < GPCRs in Oncology and Immunology The GPCR-Gαs-PKA signaling axis promotes T cell dysfunction Here, we cross-integrated large singe-cell RNA-sequencing datasets from CD8+ T cells covering 19 distinct cancer types and identified an enrichment of Gαs-coupled GPCRs on exhausted CD8+ T cells. These include EP2, EP4, A2AR, β1AR and β2AR, all of which promote T cell dysfunction. Gαs-DREADD to activate CD8-restricted Gαs signaling and show that a Gαs-PKA signaling axis promotes CD8+ T cell

activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer cell Here, we show that HRH1 is widely expressed in various cancer cell lines and cancer tissues and that that endogenously express CXCR4 and HRH1 but not in cells deficient in CXCR4 or HRH1. while histamine alone does not induce cell migration. Enhanced calcium signaling and cell migration are also observed in NCI-H23 and HeLa cells, which coexpress

expression of GPR50 promotes the proliferation, migration and autophagy of hepatocellular carcinoma cells was analyzed in HCC patients (gene expression omnibus database (GEO) (GSE45436)) and detected in HCC cell 7919, and the results showed that GPR50 was significantly up-regulated in HCC patients and CBRH-7919 cell Gpr50 cDNA was transfected into HCC cell line CBRH-7919, and we found that Gpr50 promoted the proliferation Cuifang Chang Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call

and Immunology Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells IGF-1 receptors and G protein-coupled (GPCR) signaling systems leading to mitogenic signaling in PDAC cells agonist neurotensin induced rapid activation of Src family of tyrosine kinases (SFK) within PANC-1 cells by FAK phosphorylation at Tyr576/577 and Tyr861, sensitive biomarkers of SFK activity within intact cells and suppressed the growth of Mia PaCa-2 cells xenografted into the flank of nude mice.

She received her BSc in Human Biology from King’s College London in 1997, and while her Ph.D. commenced Her research focuses on understanding the fundamental cell biological mechanisms regulating GPCR activity Her work is currently funded by Biotechnology and Biological Sciences Research Council (BBSRC), Diabetes Alejandra Tomas is a molecular cell biologist and Senior Lecturer at the Department of Metabolism, Digestion several years in Switzerland working on the study of membrane trafficking processes in pancreatic beta cells

< GPCR News < GPCRs in Oncology and Immunology A2aR on lung adenocarcinoma cells: A novel target for 2a receptor (A2aR), a typical GPCR with a high affinity for adenosine, is widely expressed on immune cells Here, we identify that A2aR is specifically expressed on tumor cells from lung adenocarcinoma (LUAD) We hypothesize that blocking A2aR on LUAD cells will inhibit the role of TAMs and control tumor growth Constructing models of TAMs and LUAD mice, we find that A2aR highly expressed on LUAD cells promotes

< GPCR News < GPCRs in Oncology and Immunology RGS20 promotes non-small cell lung carcinoma proliferation CCK8 and cell cloning were conducted to determine the proliferation ability of H1299 and Anip973 cells Further, RGS20 accelerated cell proliferation by increasing autophagy. in RGS20 knock-down cells. Conclusion: Our findings indicate that RGS20 drives NSCLC cell proliferation by triggering autophagy

< GPCR News < GPCRs in Oncology and Immunology Single cell G-protein coupled receptor profiling of Transcription Key results: Transcription factor 21 (Tcf21)+ cells that expressed 2 or 3 of Postn, Acta2 and Pdgfra Tcf21+ α-smooth muscle actin (α-SMA)+ interstitial cells accumulated in the kidneys of mice with UUO TCF21, ADGRA2, S1PR3 and ADORA2A/2B were each detectable in α-SMA+ interstitial cells in human kidneys Study of GPCRs expressed by these cells may identify new opportunities for CKD therapeutics. " Authors

induces IFN-γ but suppresses IL-2 production by inhibiting activation of pAKT pathways in primary T cells signaling molecules and the phosphatidylinositol, Ras, MAPK, and PI3 kinase pathways, leading to T cell This may explain the inhibitory impact on IL-2 production in hM3Dq/β1T cells. that activating the pAKT pathway is critical for IL-2 production in T cells." Tags GPCR; T cells; muscarinic receptor; signaling.

< GPCR News < GPCRs in Oncology and Immunology CCL5-producing migratory dendritic cells guide CCR5+ monocytes into the draining lymph nodes Published date March 21, 2023 Abstract "Dendritic cells (DCs) and monocytes capture, transport, and present antigen to cognate T cells in the draining lymph nodes (LNs) in a CCR7 Jakubzick Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call

< GPCR News < GPCRs in Oncology and Immunology TIPE proteins control directed migration of human T cells human TIPE family members, TNFAIP8 and TIPE2 were essential for directed migration of human CD4+ T cells T Cells deficient in both of these proteins completely lost their directionality. bisphosphate (PIP2) and phosphatidylinositol 3,4,5-triphosphate (PIP3) to spatiotemporally control immune cell Collectively, our work describes a new mechanistic paradigm for how human T cells integrate GPCR and

transmitting signals inside the body, which is necessary for controlling the life activities of all cells , including tumor cells [1]. nucleotides to their respective di and mono-phosphate nucleoside forms, contributing significantly to immune biology , cancer biology, and inflammation studies. ATP functions as a mighty damage-linked molecular pattern when released outside the cell, accumulating

pathway by G protein-coupled receptor 37 promotes resistance to cisplatin-induced apoptosis in non-small cell protein-coupled receptor 37 (GPR37) exhibits unknown functions in tumors, particularly in non-small-cell We detected the expression of GPR37 in NSCLC tissues and cell lines. The study explored the influence of GPR37 on tumor cell proliferation. Furthermore, we examined the effects of GPR37 on tumor cell apoptosis and invasion.

Oncology and Immunology Enterococcus-derived tyramine hijacks α2A-adrenergic receptor in intestinal stem cells disease (IBD) is characterized by dysbiosis of the gut microbiota and dysfunction of intestinal stem cells Using an engineered tyrDC-deficient Enterococcus faecalis strain and intestinal epithelial cell-specific adrenergic receptor Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call

Immunology Comparative Analysis of the GNAI Family Genes in Glioblastoma through Transcriptomics and Single-Cell regulation of actin cytoskeleton organization by the kinase effectors of Rho GTPases" and "Immune response B cell A single-cell analysis was used to assess GNAI3 expression in GBM. Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call for GPCR