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< GPCR News < GPCRs in Oncology and Immunology Biochemical pharmacology of adenylyl cyclases in cancer date October 1, 2024 Abstract "Globally, despite extensive research and pharmacological advancement, cancer Understanding the signaling pathways involved in cancer progression is essential for the discovery of The expression patterns of ACs in numerous cancers are discussed. , G protein , GPCR , Hallmarks of Cancer , cAMP signaling .

A defining hallmark of GBM is a highly acidic tumor microenvironment, which is thought to activate pro-tumorigenic Lorazepam, which has off target agonism of GPR68, is linked to worse clinical outcomes for a variety of cancers However, the role of tumor microenvironment acidification in GPR68 activation has not been assessed in cancer

< GPCR News < GPCRs in Oncology and Immunology Chemokine Physiology in Cancer Published date November In cancer, chemokines play paradoxical roles in both the directed emigration of metastatic, receptor-expressing cancer cells out of the tumor as well as immigration of tumor infiltrating immune cells that culminate Facets of chemokine physiology across discrete cancer immune phenotypes are contrasted to existing chemokine-centered therapies in cancer.

Published date November 1, 2022 Abstract Blocked cellular differentiation is a critical pathologic hallmark

< GPCR News < GPCRs in Oncology and Immunology Short-chain fatty acids and cancer Published date December the microbiota, serve as crucial links between the diet, gut microbiota, metabolism, immunity, and cancer influencing tumor progression highlights the potential of targeting SCFA-mediated cellular processes for cancer Authors Shan Li, Yixin Duan, Shudi Luo, Fangxin Zhou, Qingang Wu, Zhimin Lu Tags acetate , butyrate , cancer

Indeed, gut microbiota dysbiosis and metabolomic profile alterations, are hallmarks of IBD.

< 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 The landscape of cancer-rewired GPCR signaling axes Published

< GPCR News < GPCRs in Oncology and Immunology Role and recent progress of P2Y12 receptor in cancer development P2Y12R activation can promote platelet aggregation and adhesion to cancer cells, promote tumor angiogenesis immune microenvironment (TIME) and tumor drug resistance, which is conducive to the progression of cancers cancer. However, a new study suggests that long-term use of P2Y12R inhibitors may increase the risk of cancer

GPCR News < GPCRs in Oncology and Immunology From odor to oncology: non-canonical odorant receptors in cancer sensory perception, emerging evidence suggests a compelling interplay between odorant receptors and cancer types, suggesting their contributions to cancer progression. The roles of these non-canonical chemoreceptors in cancer are complex, with some receptors promoting tumorigenesis and others acting as tumor-suppressing factors upon activation, depending on the cancer

Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule G Proteins and GPCRs in Cancer Department of Pharmacology, School of Medicine, and Associate Director for Basic Science at the Moores Cancer treatments, and to identify novel multimodal strategies to enhance the response to cancer immunotherapies Silvio Gutkind on the web Gutkind Lab – UC San Diego Moores Cancer Center Gutkind Lab publications Pubmed LinkedIn Twitter UCSD Moores Cancer Center Dr.

News < GPCRs in Oncology and Immunology Agonists of galanin subtype 2 receptor may prevent pancreatic cancer and agonists of angiotensin II type 2 receptor may prevent colorectal cancer Published date June 24, of colorectal carcinoma (CRC) is better than that of PDAC, it still is the second-leading cause of cancer receptor inhibited the growth of GAL2 receptor-expressing patient-derived xenografts (PDX) of pancreatic cancer lanthionine-constrained agonist of angiotensin II type 2 (AT2) receptor inhibited PDX of colorectal cancer

Immunology Involvement of Protease-Activated Receptor2 Pleckstrin Homology Binding Domain in Ovarian Cancer Fallopian Tubes and Drug Design Published date January 22, 2024 Abstract "Studying primordial events in cancer While the involvement of G-protein-coupled receptors (GPCRs) in cancer is growing, GPCR-based therapies PAR2 expression in FTs may serve as an early prediction sensor for ovarian cancer. serve as a powerful medicament in STICs and ovarian cancer.

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. Rottapel’s research interests lies in the elucidation of signal transduction pathways in cancer, immune He has focussed on developing a comprehensive map of ovarian cancer essential genes using whole genome

in Oncology and Immunology Metabolic crosstalk: Extracellular ATP and the tumor microenvironment in cancer their respective di and mono-phosphate nucleoside forms, contributing significantly to immune biology, cancer

< 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 Purinergic GPCR-integrin interactions drive pancreatic cancer P2RY2 presents as the purinergic gene with the strongest association with hypoxia, the highest cancer Moreover, receptor-integrin interactions were required for effective downstream signalling, leading to cancer This work elucidates a novel GPCR-integrin interaction in cancer invasion, highlighting its potential Ariana Samadi , Hemant M Kocher , Sabrina Simoncelli , Peter J McCormick , Richard Philip Grose Tags 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

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

Minireview: functional roles of tissue kallikrein, kinins, and kallikrein-related peptidases in lung cancer Published date July 3, 2023 Abstract "Despite campaigns and improvements in detection and treatment, 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,

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.

< 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

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

< 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

< GPCR News < GPCRs in Oncology and Immunology Lactate receptor GPR81 drives breast cancer growth and DLL4 Published date November 22, 2023 Abstract " Background: The lactate receptor GPR81 contributes to cancer 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 lactate and 3D growth in breast cancer spheroids.

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

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.

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.