and Immunology [1,2,4]Triazolo[1,5-c]pyrimidines as Tools to Investigate A3 Adenosine Receptors in Cancer Cell Lines Published date September 7, 2023 Abstract "A3 adenosine receptor is an interesting target that showed controversial roles in cancer. Compound 20 has been tested on both A3 adenosine receptor positive cancer cell lines (CHO-A3AR transfected , THP1 and HCCT26) and in A3 negative cancer cell lines, showing no effect on the latter and a proliferative

GPCRs in Oncology and Immunology Autocrine proteinase-activated receptor signaling in PC3 prostate cancer cells Published date June 29, 2023 Abstract "Proteinase-activated receptors (PARs) are G protein-coupled 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 of PAR1 promotes PC3 cell migration and suppresses cell proliferation, whereas PAR2 deficiency showed

overexpressed in various types of cancer and is involved in several cancer phenotypes including tumor Here, we show that HRH1 is widely expressed in various cancer cell lines and cancer tissues and that coexpression of CXCR4 and HRH1 is associated with poor prognosis in breast cancer. 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 The landscape of cancer-rewired GPCR signaling axes Published 2024 Abstract "We explored the dysregulation of G-protein-coupled receptor (GPCR) ligand systems in cancer Multiple GPCRs are differentially regulated together with their upstream partners across cancer subtypes cell drug screens, which we further validated. , cancer cell lines , cell-cell communication , drug repurposing , personalized medicine , signaling

GPCRs in Oncology and Immunology Vasoactive intestinal peptide receptor 2 signaling promotes breast cancer However, the pathophysiological role of increased VIPR2 in the proliferation of breast cancer cells remains In this study, we found that VIPR2 overexpression in MCF-7 and MDA-MB-231 cells, human breast cancer cell lines, promoted cell proliferation. Increased VIPR2 also exacerbated intraperitoneal proliferation of breast cancer MDA-MB-231 cells in a

the NPYRs to interrogate their functional relevance in breast cancer. cell lines MDA-MB-231 and MCF7. proliferation, cell migration and invasion, and spheroid growth and invasion. There were some discrepancies in the responses of each cell line to the isoform-specific antagonists Tags Breast cancer , GPCR , Hypoxia , NPY , Neuropeptide .

< GPCRs in Oncology and Immunology GPR143 controls ESCRT-dependent exosome biogenesis and promotes cancer GPR143 is elevated in multiple cancers, and quantitative proteomic and RNA profiling of exosomes in human cancer cell lines showed that the GPR143-ESCRT pathway promotes secretion of exosomes that carry unique cell motility/invasion through the integrin/FAK/Src pathway. cell motility. " Authors Yu Jin Lee , Kyeong Jin Shin , Hyun-Jun Jang , Jin-Sun Ryu , Chae Young Lee

Methods: GPR81 was stably knocked down (KD) in MCF-7 human breast cancer cells which were subjected to Key findings were additionally studied in other breast cancer cell lines and in mammary epithelial cells lactate and 3D growth in breast cancer spheroids. in the same cell clusters. Conclusions: GPR81 supports breast cancer aggressiveness, and in MCF-7 cells, this occurs at least in

GPCRs in Oncology and Immunology Unveiling G-protein coupled receptors as potential targets for ovarian cancer analysis to in vitro validation Published date July 27, 2024 Abstract "Genetic heterogeneity in ovarian cancer To address the genetic heterogeneity of ovarian cancer, a future personalised approach could include the identification of unique GPCRs expressed in cancer biopsies, matched with personalised GPCR-targeted Subsequently, primary ovarian cancer cells derived from ascites and ovarian cancer cell lines were used

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 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 , Hua Xiao Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR News Call

Likewise, lysophosphatidic acid receptor 1 (LPA1) is implicated in cancer cell proliferation and migration breast cancer cell line MDA-MB-231. LPA or alkyl-OMPT inhibited CXCL12-induced migration in various cancer cells that endogenously express MDA-MB-231 cells but not in LPA1-deficient cells. have been evidenced across various cell lines.

protein-coupled receptors (GPCRs), enhancing proliferation, adhesion, and migration in many types of cancer cells. Our group previously reported that LPA induces production of CCN1 protein in human prostate cancer cell lines within 2-4 h. In these cells, the mitogenic activity of LPA is mediated by LPA Receptor 1 (LPAR1), a GPCR.

PIE-FCCS can resolve membrane protein density, diffusion, and multimerization state in live cells at We probed CXCR4 and β2AR homo- and heteromultimerization in model cell lines and found that CXCR4 assembles into multimeric complexes larger than dimers in MDA-MB-231 human breast cancer cells and in HCC4006 human lung cancer cells. These results suggest that CXCR4-β2AR heteromers are present in human cancer cells and that GPCR multimerization

Caroline Formstone Abstract "Breast cancer is the most common form of cancer amongst women. The impact of CELSR1 on cancer progression, however, is unclear. and cell-matrix contacts. Notably, our pilot data from luminal-type breast cancer cell lines representative of breast carcinomas To test this hypothesis, we created WNT-like MB cell lines stably expressing tet-on wild-type BAI3 or

GPCR News < GPCRs in Oncology and Immunology Purinergic GPCR-integrin interactions drive pancreatic cancer cell invasion Published date March 21, 2023 Abstract " Pancreatic ductal adenocarcinoma (PDAC) continues cell-specific expression and the strongest impact on overall survival. cell invasion. biology , cell biology , human.

< GPCR News < GPCRs in Oncology and Immunology GPR176 Promotes Cancer Progression by Interacting with G Protein GNAS to Restrain Cell Mitophagy in Colorectal Cancer Published date March 11, 2023 Abstract belongs to the G protein-coupled receptor superfamily, which responds to external stimuli and regulates cancer progression, but its role in colorectal cancer (CRC) remains unclear. In the present study, expression analyses of GPR176 are performed in patients with colorectal cancer.

< GPCR News < GPCRs in Oncology and Immunology Chemokine Physiology in Cancer Published date November Chemokines are chemotactic cytokines whose canonical functions govern movement of receptor expressing cells cancer cells out of the tumor as well as immigration of tumor infiltrating immune cells that culminate therapies in cancer. Authors Donovan Drouillard, Brian T Craig, Michael B Dwinell Tags Chemokine receptor; cell migration;

< GPCR News < GPCRs in Oncology and Immunology Molecular characterization of breast cancer cell pools PR is an important prognostic factor in breast cancer. cells. cells. cells.

and Immunology Systems Pharmacodynamic Model of Combination Gemcitabine and Trabectedin in Pancreatic Cancer Cells. prior study, we reported the synergistic cytotoxic effects of gemcitabine and trabectedin on pancreatic cancer cells. analysis was performed, and a system pharmacodynamics model (SPD) was developed to capture pancreatic cancer

and cancer immunotherapy failure Published date June 12, 2023 Abstract "Immune checkpoint blockade ( ICB) targeting PD-1 and CTLA-4 has revolutionized cancer treatment. However, many cancers do not respond to ICB, prompting the search for additional strategies to achieve 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.

cells by targeting PAR-1 Published date June 21, 2024 Abstract "We have purified Peptidase M84 from 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 NPFF stimulates human ovarian cancer cell invasion by Epithelial ovarian cancer (EOC) is a leading cause of death among gynecological malignancies. 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 Fang , Peter C K Leung , Jung-Chien Cheng Tags Invasion , MMP-9 , NPFFR2 , Neuropeptide FF , Ovarian cancer

lung cancer Published date September 21, 2023 Abstract "Objectives: Lung cancer is a major public health concern and represents the most common cause of cancer-related death worldwide. lung cancer (NSCLC) METHODS: We explored the expression and prognosis of GPR37 in NSCLC through TCGA We detected the expression of GPR37 in NSCLC tissues and cell lines. The study explored the influence of GPR37 on tumor cell proliferation.

Oncology and Immunology Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer adenocarcinoma (PDAC) remains an aggressive disease that is expected to become the second cause of cancer siRNA-mediated knockdown of YES1, and transfection of epitogue-tagged YAP mutants in PANC-1 and Mia PaCa-2 cancer cells, models of the aggressive squamous subtype of PDAC. and suppressed the growth of Mia PaCa-2 cells xenografted into the flank of nude mice.

< GPCR News < GPCRs in Oncology and Immunology Biochemical pharmacology of adenylyl cyclases in cancer Understanding the signaling pathways involved in cancer progression is essential for the discovery of The precise mechanisms by which ACs contribute to cancer cell proliferation and invasion are not well The expression patterns of ACs in numerous cancers are discussed. , G protein , GPCR , Hallmarks of Cancer , cAMP signaling .

Immunology PAXIP1-AS1 is associated with immune infiltration and predicts poor prognosis in ovarian cancer antisense RNA 1 (PAXIP1-AS1) was found to promote proliferation, migration, EMT, and apoptosis of ovarian cancer (OC) cells in OC cell lines, but the relationship between PAXIP1-AS1 expression and clinical characteristics QRT-PCR was used to validate the expression of PAXIP1-AS1 in OC cell lines. PAXIP1-AS1 was significantly downregulated in OC cell lines compared with IOSE29 cell line.

Minireview: functional roles of tissue kallikrein, kinins, and kallikrein-related peptidases in lung cancer on tumor cells, such as GPCR-family kinin receptors, and proteases that control tumor progression, such , such as prostate and ovarian cancer, facilitating the invasive and metastatic capacity of tumor cells The expression levels of KLKs in this neoplasm are modulated by the secretome of the different cell types present in the tumor microenvironment, the cancer subtype and the tumor stage, among others.

to schedule Inhibition of Relaxin Autocrine Signaling Confers Therapeutic Vulnerability in Ovarian Cancer Rottapel is a Senior Scientist at the Princess Margaret Cancer Centre where he holds the Amgen Chair for Cancer Research. and bone cells. The Rottapel lab has shown that 3BP2 has pleiotrophic function controlling bone homeostasis, immune cell