between GPR37 gene expression and the clinicopathological factors, patient prognosis, tumor-infiltrating immune clinical relevance, and molecular function of GPR37 in glioma using TCGA, STRING, cBioPortal, Tumor Immunity Besides, the "ssGSEA" algorithm was conducted to estimate immune cells infiltration abundance, with ' Furthermore, GPR37 was positively correlated with various immune checkpoints (ICPs). Lai , Huaidong Peng , Yanbin Ke , Zhaotao Wang , Yezhong Wang Tags GPR37 , M2 macrophages , glioma , immune

This pathway is implicated in mechanisms related to many diseases, such as cancer, psoriasis, multiple The CCR6/CCL20 axis plays a fundamental role in immune homeostasis and activation. Tags CCR6 , GPCRs , Th17 cells , antibody , immune system , inflammation , therapy .

< 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 findings provide a mechanism for regulating the exosomal proteome and demonstrate its ability to promote cancer , Sun-Young Kong , Taejoon Kwon , Pann-Ghill Suh , Young Chan Chae Tags GPR143 , HRS , MVB , breast cancer

< GPCR News < GPCRs in Oncology and Immunology Pan-cancer functional analysis of somatic mutations in GPCRs) are the most frequently exploited drug target family, moreover they are often found mutated in cancer We explored cancer-related mutation patterns in all GPCR classes combined and individually. A Two-Entropy Analysis confirmed the correlation between residue conservation and cancer-related mutation families, but also discovered novel GPCRs which had not been linked to cancer before such as the P2Y

Minireview: functional roles of tissue kallikrein, kinins, and kallikrein-related peptidases in lung cancer One approach to treating patients suffering from lung cancer is to target surface receptors overexpressed , such as prostate and ovarian cancer, facilitating the invasive and metastatic capacity of tumor cells Since lung cancer is often diagnosed in advanced stages, our efforts should focus on early diagnosis, Furthermore, their modulation could be considered as a promising approach in lung cancer therapeutics

< GPCR News < GPCRs in Oncology and Immunology Ultrasensitive dose-response for asbestos cancer risk is expected for damage that accumulates in proportion to dose, as hypothesized for increased risk of cancer relation to genotoxic dose according to the multistage somatic mutation/clonal-expansion theory of cancer Mesothelioma and lung cancer induced by exposure to carcinogenic (e.g., certain asbestos) fibers in humans A recent Inflammation Somatic Mutation (ISM) theory of cancer posits instead that tissue-damage-associated

and Immunology Investigating isoform switching in RHBDF2 and its role in neoplastic growth in breast cancer Published date November 1, 2022 Abstract Background: Breast cancer is the second leading cause of cancer-related In the past, studies predicting therapeutic drug targets for cancer therapy focused on the assumption Therefore, there is always an immense need to find promising and novel anti-cancer drug targets. Tags Breast cancer; EGFR; ERAD; RHBDF2; TACE; iRhom2.

< GPCR News < GPCRs in Oncology and Immunology G protein coupled receptor transcripts in human immune

GPCRs in Oncology and Immunology Autocrine proteinase-activated receptor signaling in PC3 prostate cancer 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

Deciphering a GPCR-lncRNA-miRNA Nexus: Identification of an Aberrant Therapeutic Target in Ovarian Cancer Published date April 18, 2024 Abstract "Ovarian cancer ranks as a leading cause of mortality among gynecological Previous studies have identified the pivotal role of Lysophosphatidic acid (LPA)-signaling in ovarian cancer UCA1 expression inversely correlates with survival outcomes and therapy response in ovarian cancer clinical xenografts, demonstrating the therapeutic potential of targeting LPAR-UCA1-let-7 axis in ovarian cancer

GPCRs in Oncology and Immunology The β2-adrenergic receptor associates with CXCR4 multimers in human cancer 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

Patients' data on HCC were sourced from the Liver Hepatocellular Carcinoma-Japan (LIRI-JP) and The Cancer The tumor immune dysfunction and exclusion (TIDE) algorithm was utilized to evaluate immune infiltration immunotherapy and common antitumor drugs was predicted via the database Genomics of Drug Sensitivity in Cancer

Expanding role of CXCR2 and therapeutic potential of CXCR2 antagonists in inflammatory diseases and cancers is G protein-coupled receptor (GPCR) and plays important roles in various inflammatory diseases and cancers , including chronic obstructive pulmonary disease (COPD), atherosclerosis, asthma, and pancreatic cancer structure-activity relationships and clinical significance of CXCR2 antagonists in inflammatory diseases and cancers Authors Yishi Xie , Wenbin Kuang , Dawei Wang , Kai Yuan , Peng Yang Tags CXCR2 , CXCR2 antagonist , Cancer

< GPCR News < GPCRs in Oncology and Immunology Drosophila cytokine GBP2 exerts immune responses and regulates Here, we demonstrate that GBP2 replicates the GBP1-mediated cellular immune response from Drosophila Our finding revealed that Drosophila GBP1 and GBP2 control immune responses as well as their own expression

< GPCR News < GPCRs in Oncology and Immunology Ovarian cancer G protein-coupled receptor 1 (OGR1) deficiency In this setting, OGR1 KO mice displayed an increased activation of the immune system and a higher production

Immunology Involvement of Protease-Activated Receptor2 Pleckstrin Homology Binding Domain in Ovarian Cancer While the involvement of G-protein-coupled receptors (GPCRs) in cancer is growing, GPCR-based therapies FTs, the origin of ovarian cancer, are known to express genes of serous tubal intraepithelial carcinoma PAR2 expression in FTs may serve as an early prediction sensor for ovarian cancer. serve as a powerful medicament in STICs and ovarian cancer.

and Immunology Mechanistic exploration of bioactive constituents in Gnetum gnemon for GPCR-related cancer integral membrane proteins that have gained considerable attention as drug targets, particularly in cancer Gnetum gnemon (GG) for the development of of pharmaceuticals targeting GPCRs within the context of cancer We retrieved targets for GG-derived compounds and GPCRs-related cancer from databases. Survival analysis established the clinical prognostic relevance of identified hub genes in cancer.

Oncology and Immunology Small-molecule targeting of GPCR-independent noncanonical G-protein signaling in cancer GIV/Girdin has emerged as a prototypical non-GPCR activator of G proteins that promotes cancer metastasis blocking noncanonical G-protein signaling in tumor cells and inhibiting proinvasive traits of metastatic cancer Tags G protein , GPCR , cancer , drug discovery .

< GPCR News < GPCRs in Oncology and Immunology The Effect of Cancer-Associated Mutations on Ligand Binding regulating mood, appetite, and reproductive behavior, it has been identified as a potential target for cancer In this study, we aimed to investigate the effects of cancer patient-derived 5-HT2C receptor mutations sequencing data from the Genomic Data Commons data portal (GDC), we selected 12 mutations from multiple cancer P van Westen, Erik H J Danen, Laura H Heitman Tags 5-HT(2C) receptor , G protein-coupled receptor , cancer

< GPCR News < GPCRs in Oncology and Immunology Lactate receptor GPR81 drives breast cancer growth and Here, we investigate the roles of GPR81 in three-dimensional (3D) and in vivo growth of breast cancer Methods: GPR81 was stably knocked down (KD) in MCF-7 human breast cancer cells which were subjected to Results: GPR81 was upregulated in multiple human cancer types and further upregulated by extracellular lactate and 3D growth in breast cancer spheroids.

This axis is linked to diseases like HIV/SIV, cancer, and COVID-19. Together, these highlight that the CXCL16-CXCR6 axis is pivotal in host immunity. ITGAE, CXCL16, and CXCR6 in chickens may have altered CD8 TRM cell abundance, with implications for immunity

Immunology Pharmacological inhibition of neuropeptide Y receptors Y1 and Y5 reduces hypoxic breast cancer This abundance is exploited for cancer imaging, but there is interest in pharmacological inhibition of the NPYRs to interrogate their functional relevance in breast cancer. Therefore, these antagonists may aid in the development of novel cancer therapeutics and patient-based Tags Breast cancer , GPCR , Hypoxia , NPY , Neuropeptide .

Simultaneous activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer and is involved in several cancer phenotypes including tumor growth, survival, and metastasis. The roles of histamine and histamine receptor H1 (HRH1) in cancer pathogenesis remain controversial. 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.

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 [1,2,4]Triazolo[1,5-c]pyrimidines as Tools to Investigate A3 Adenosine Receptors in Cancer 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 Karl-Norbert Klotz , Sabrina Pacor , Stefano Moro , Giampiero Spalluto Tags A3 adenosine receptor , Cancer

< GPCR News < GPCRs in Oncology and Immunology Molecular characterization of breast cancer cell pools Abstract "Background: About one-third of patients with estrogen receptor alpha (ERα)-positive breast cancer PR is an important prognostic factor in breast cancer. New evidence has shown that progesterone (P4) has an anti-proliferative effect in ERα-positive breast cancer However, the role of PR in breast cancer is only poorly understood.

GPCRs in Oncology and Immunology Vasoactive intestinal peptide receptor 2 signaling promotes breast cancer Increased VIPR2 mRNA expression and/or VIPR2 gene copy number has been documented in several cancers 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 Increased VIPR2 also exacerbated intraperitoneal proliferation of breast cancer MDA-MB-231 cells in a

Metallo-protease Peptidase M84 from Bacillusaltitudinis induces ROS-dependent apoptosis in ovarian cancer had no discernible impact on normal cell survival, but it specifically induced apoptosis in ovarian cancer 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. This established Peptidase M84 as a drug candidate for receptor mediated targeted-therapy of ovarian cancer