< 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 therapies in cancer. Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

Published date October 1, 2024 Abstract "Globally, despite extensive research and pharmacological advancement , cancer remains one of the most common causes of mortality. The expression patterns of ACs in numerous cancers are discussed. , G protein , GPCR , Hallmarks of Cancer , cAMP signaling . Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

Rottapel is a Senior Scientist at the Princess Margaret Cancer Centre where he holds the Amgen Chair for Cancer Research. University, the NIH and UCLA, he pursued his postdoctoral studies with Allan Bernstein at the Lunenfeld Research Rottapel’s research interests lies in the elucidation of signal transduction pathways in cancer, immune Robert Rottapel on the web The Rottapel Lab Ontario Institute for Cancer Research University of Toronto

< 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 cancer. However, a new study suggests that long-term use of P2Y12R inhibitors may increase the risk of cancer Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

< 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 , cancer cell lines , cell-cell communication , drug repurposing , personalized medicine , signaling Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 His research team has pioneered the study of G proteins and G protein coupled receptors (GPCRs) in human Silvio Gutkind on the web Gutkind Lab – UC San Diego Moores Cancer Center Gutkind Lab publications Pubmed LinkedIn Twitter UCSD Moores Cancer Center Dr.

< 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 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. Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

GPCR News < GPCRs in Oncology and Immunology From odor to oncology: non-canonical odorant receptors in 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 Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

< 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. families, but also discovered novel GPCRs which had not been linked to cancer before such as the P2Y Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 lanthionine-constrained agonist of angiotensin II type 2 (AT2) receptor inhibited PDX of colorectal cancer Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

< 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 , Sun-Young Kong , Taejoon Kwon , Pann-Ghill Suh , Young Chan Chae Tags GPR143 , HRS , MVB , breast cancer Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

< 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 Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 Authors Yishi Xie , Wenbin Kuang , Dawei Wang , Kai Yuan , Peng Yang Tags CXCR2 , CXCR2 antagonist , Cancer Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 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 Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 xenografts, demonstrating the therapeutic potential of targeting LPAR-UCA1-let-7 axis in ovarian cancer Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 Therefore, there is always an immense need to find promising and novel anti-cancer drug targets. Tags Breast cancer; EGFR; ERAD; RHBDF2; TACE; iRhom2. Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

power of many: Multilevel targeting of representative chemokine and metabolite GPCRs in personalized cancer highlights five GPCRs able to orchestrate tumor immunobiology at three main levels: tumor immunity, cancer Authors Donato Inverso, Carlotta Tacconi, Serena Ranucci, Marco De Giovanni Tags Angiogenesis , Cancer Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 PAR2 expression in FTs may serve as an early prediction sensor for ovarian cancer. serve as a powerful medicament in STICs and ovarian cancer. Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 . Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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. Tags Breast cancer , GPCR , Hypoxia , NPY , Neuropeptide . Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

< 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 lactate and 3D growth in breast cancer spheroids. Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

< GPCR News < GPCRs in Oncology and Immunology Functional Assessment of Cancer-Linked Mutations in Sensitive Genetic variants in RGS proteins are associated with many diseases, including cancers, although the impact COSMIC cancer database were selected to define the functional phenotype. classifies loss-of-function mutations in RGS proteins than other databases thereby offering a valuable new research Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 Subsequently, primary ovarian cancer cells derived from ascites and ovarian cancer cell lines were used Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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. Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research

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 Karl-Norbert Klotz , Sabrina Pacor , Stefano Moro , Giampiero Spalluto Tags A3 adenosine receptor , Cancer Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders, Drugs, and more Methods & Updates in GPCR Research