atypical receptor ACKR3 both respond to CXCL12 but induce different effector responses to regulate cell While CXCR4 couples to G proteins and directly promotes cell migration, ACKR3 is G protein-independent Authors Christopher T Schafer, Raymond F Pauszek 3rd, Martin Gustavsson, Tracy M Handel, David P Millar single-molecule FRET Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call

implied by new inflammation-mutation model Published date August 1, 2023 Abstract "Alterations in complex cellular tissue-damage-associated inflammation that epigenetically recruits, activates and orchestrates stem cells Author Kenneth T Bogen Tags Asbestos , Cytotoxicity , Inflammation , Lung cancer , Mesothelioma , Mutation Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call for GPCR

Many ADGRs are autoproteo-lytically cleaved at the GPCR proteolysis site (GPS), an HXS/T motif within extracellular regions (ECRs) with nine cadherin repeats and a variety of adhesion domains which couple cell CELSRs regulate planar cell polarity, including the closure of the neural tube. Despite numerous cell and animal studies, molecular details on CELSR proteins are sparsely available, We assign the N-terminal CADH1-8 module as necessary for cell adhesion and we show the C-terminal CAHD9

inflammation is characterized by overexpression and heightened activity of type 2 cytokines, mediators and cells FeNO , Fractional exhaled nitric oxide , G-protein-coupled receptor , GPCR , Group 2 innate lymphoid cell , IL-31RA , IL-33R , IL-4Rα , IL-5Rα , ILC , ILC2 , IRF1 , IgE , Immunoglobulin E , Innate lymphoid cell Sialic-acid-binding immunoglobulin-like lectin 8 , Signal transducer and activator of transcription , Substance P , T helper type 2 cell , TRP , TRPA1 , TRPM4 , TRPM8 , TRPV1 TRPV4 , TSLP , TSLPR , Th2 , Thymic stromal

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.

key role in supporting the growth, maintenance, and repair of almost all tissues by responding to the cellular Authors Nidhi V Dwivedi , Souvik Datta , Karim El-Kersh , Ruxana T Sadikot , Apar K Ganti , Surinder targeting Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call

progression in MCF-7 cells Published date March 1, 2024 Abstract "Vasoactive intestinal peptide (VIP In this study, we examined the role of VIPR2 in cell cycle progression. in MCF-7 cells. The percentage of cells in the S-M phase was decreased in MCF-7 cells treated with KS-133. In MCF-7 cells stably-expressing VIPR2, KS-133 decreased PI3K activity and cAMP levels.

< 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 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 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

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

< 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

G protein βγ subunits inhibitor, suppresses the TGF-α-induced migration of hepatocellular carcinoma cells Abstract "G protein-coupled receptor (GPCR) signaling regulates a wide range of pathophysiological cell transforming growth factor-α (TGF-α) induces the migration of human hepatocellular carcinoma (HCC) HuH7 cells This study aims to determine whether Gβγ subunits regulate the TGF-α-induced migration of HCC HuH7 cells Gallein significantly reduced the TGF-α-induced cell migration.

< 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 miR-19a may function as a biomarker of oral squamous cell Using a transcriptomic analysis of over 37,000 nuclei, we identified twelve distinct clusters of cells corresponding to temperature-sensing arista neurons, humidity-sensing sacculus neurons, and support cells We found that each cell type could be characterized by a unique expression profile of ion channels, GPCR signaling molecules, synaptic vesicle cycle proteins, and cell adhesion molecules.

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.

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.

Metallo-protease Peptidase M84 from Bacillusaltitudinis induces ROS-dependent apoptosis in ovarian cancer cells This metallo-protease had no discernible impact on normal cell survival, but it specifically induced apoptosis in ovarian cancer cells. PAR-1, a GPCR which is reported to be overexpressed in ovarian cancer cells, was identified as a target This evoked apoptotic death of the ovarian cancer cells through the intrinsic route.

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 Purinergic GPCR-integrin interactions drive pancreatic cancer cell P2RY2 presents as the purinergic gene with the strongest association with hypoxia, the highest cancer cell-specific receptor-integrin interactions were required for effective downstream signalling, leading to cancer cell Hemant M Kocher , Sabrina Simoncelli , Peter J McCormick , Richard Philip Grose Tags cancer biology , cell Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call for GPCR

in Oncology and Immunology Autocrine proteinase-activated receptor signaling in PC3 prostate cancer cells Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call for GPCR

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 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

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 Dynamic Phosphoproteomics of BRS3 Activation Reveals the Hippo Signaling Pathway for Cell The lung cancer cell line H1299-BRS3 was treated with MK-5046, an agonist of BRS3, for different durations Harvested cellular proteins were digested and phosphopeptides were enriched by immobilized titanium ( dephosphorylation and nucleus localization of the Yes-associated protein (YAP), and its association with cell Our data collectively demonstrate that BRS3 activation contributes to cell migration through downregulation

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 Noopur Thakur Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call