< 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.

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.

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.

< 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.

< 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 Functional Assessment of Cancer-Linked Mutations in Sensitive Genetic variants in RGS proteins are associated with many diseases, including cancers, although the impact Intolerant and tolerant-control residues that overlap with pathogenic cancer mutations reported in the COSMIC cancer database were selected to define the functional phenotype. , including cancer-linked mutations in regulator of G protein signaling (RGS) proteins.

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 .

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

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

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

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

< GPCRs in Oncology and Immunology The GPCR-Gαs-PKA signaling axis promotes T cell dysfunction and cancer June 12, 2023 Abstract "Immune checkpoint blockade (ICB) targeting PD-1 and CTLA-4 has revolutionized cancer However, many cancers do not respond to ICB, prompting the search for additional strategies to achieve we cross-integrated large singe-cell RNA-sequencing datasets from CD8+ T cells covering 19 distinct cancer

GPCRs in Oncology and Immunology Regulator of G protein signaling 16 restrains apoptosis in colorectal cancer disrupting TRAF6-TAB2-TAK1-JNK/p38 MAPK signaling Published date June 21, 2024 Abstract "Colorectal cancer (CRC) remains a major global cause of cancer-related mortality, lacking effective biomarkers and therapeutic modulators play essential role within regulating downstream signaling of GPCR receptors, with function in cancers

guanylate kinase (MAGUK) scaffold protein, and protein kinase A anchoring protein (AKAP) 5 in MCF7 breast cancer β1-adrenergic receptor (β1AR) are G protein-coupled receptors (GPCR) that are implicated in breast cancer MCF7 breast cancer cells express GPR30, β1AR, MAGUKs, and AKAP5 in the plasma membrane, and co-immunoprecipitation Stephen Serafin , Tobias Schmidt , Björn Olde , Kathleen M Caron , L M Fredrik Leeb-Lundberg Tags Breast cancer

< GPCR News < GPCRs in Oncology and Immunology Esophageal and gastric cancer incidence trends in Golestan June 29, 2023 Abstract "Golestan province in the northeast of Iran is part of the Asian esophageal cancer belt and is known as a high-risk area for esophageal (EC) and gastric cancers (GC). on incident cases of EC and GC during 2004 to 2018 were obtained from the Golestan Population-based Cancer

and Immunology Systems Pharmacodynamic Model of Combination Gemcitabine and Trabectedin in Pancreatic Cancer prior study, we reported the synergistic cytotoxic effects of gemcitabine and trabectedin on pancreatic cancer analysis was performed, and a system pharmacodynamics model (SPD) was developed to capture pancreatic cancer Straubinger , William J Jusko Tags Systems Pharmacodynamic , drug combination , gemcitabine , pancreatic cancer

< GPCR News < GPCRs in Oncology and Immunology GPR37 promotes colorectal cancer against ferroptosis by reprogramming lipid metabolism via p38-SCD1 axis Published date September 21, 2024 Abstract "Colorectal cancer Further tests showed that GPR37 protects cancer cells from ferroptosis by upregulating SCD1 expression

< GPCR News < GPCRs in Oncology and Immunology Colorectal cancer incidence trends in Golestan, Iran: the effects of factors including age, birth year (cohort) and diagnosis year (period) on colorectal cancer Methods: We obtained data on incidence cases of CRC from the Golestan Population-based Cancer Registry Weiderpass , Gholamreza Roshandel , Freddie Bray , Reza Malekzadeh Tags Age-Period-Cohort model , Colorectal Cancer

coupled receptors (GPCRs) in breast cancer, and his interest in pancreatic cancer. as a potential drug target due to its high expression in triple negative breast cancer. Mike then transitioned to pancreatic cancer, questioning why genes are dysregulated in cancer, which led him to explore different aspects of gene regulation and its relation to cancer progression. fibroblasts and is crucial for their function, leading to complications in cancer patients.

protein-coupled receptor 37 promotes resistance to cisplatin-induced apoptosis in non-small cell 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. protein-coupled receptor 37 (GPR37) exhibits unknown functions in tumors, particularly in non-small-cell lung cancer

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

A large component of his work is centered around dysregulated signaling in cancer and the development of novel mechanism-based cancer therapies. Silvio Gutkind on the web Gutkind Lab – UC San Diego Moores Cancer Center Gutkind Lab publications More J Silvio Gutkind on LinkedIn Gutkind Lab on Twitter UCSD Moores Cancer Center Dr.

Therefore, GPCRs are potential targets for cancer immunotherapy. Finally, we review the progress of clinical trials of GPCR-targeted drugs for cancer treatment, which GPCRs may shed light on the mechanisms underlying tumor progression and provide a novel perspective on cancer Authors Guang-Hong Qiu, Bin Yu, Mei Ma Tags GPCRs , cancer immune checkpoints , cancer immunotherapy

GPCR News < GPCRs in Oncology and Immunology A2aR on lung adenocarcinoma cells: A novel target for cancer

Published date November 15, 2023 Abstract "Epstein-Barr virus (EBV) is the oncogenic driver of multiple cancers However, the underlying mechanism of virus-cancer immunological interaction during disease pathogenesis as immune-inflamed, -deficient, and -desert phenotypes, in association with different setpoints of cancer-immunity expression of chemokine receptor-1 (CCR1) on malignant and immunosuppressive cells modulated virus-cancer GPCR-mediated malignant progression and translated sensors of viral molecules into EBV-specific anti-cancer

In this episode, Silvio discusses G protein signaling in the context of cancer, immunotherapies, and J Silvio Gutkind on LinkedIn Gutkind Lab – UC San Diego Moores Cancer Center Gutkind Lab publications Gutkind Lab on Pubmed Gutkind Lab on Twitter UCSD Moores Cancer Center Dr.