< 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 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.

< 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 Remarkably, we identified many such axes across several cancer molecular subtypes, including many involving , cancer cell lines , cell-cell communication , drug repurposing , personalized medicine , signaling

< 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

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

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,

< 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.

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

< 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.

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

< 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. Identified intolerant residues with reported cancer-linked mutations RGS14-R173C/H and RGS4-K125Q/E126K

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 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

< 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

receptor-related gene signature through bioinformatics analysis to construct a risk model for ovarian cancer prognosis Published date June 18, 2024 Abstract " Background: Ovarian cancer (OV) is a common malignant Method: We downloaded data from The Cancer Genome Atlas (TCGA) and Gene Expression Omnibus (GEO) databases Li, Chunfang Ha Tags G protein-coupled receptor , Immune infiltration , Molecular marker , Ovarian 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.

< 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. Fang , Peter C K Leung , Jung-Chien Cheng Tags Invasion , MMP-9 , NPFFR2 , Neuropeptide FF , Ovarian cancer

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

Oncology and Immunology Expression prevalence and dynamics of GPCR somatostatin receptors 2 and 3 as cancer

CXC chemokine receptor 4 (CXCR4) and its ligand CXCL12, both of which are overexpressed in many cancers Likewise, lysophosphatidic acid receptor 1 (LPA1) is implicated in cancer cell proliferation and migration We observed that CXCR4 forms heteromers with LPA1 in recombinant HEK293A cells and the human breast cancer LPA or alkyl-OMPT inhibited CXCL12-induced migration in various cancer cells that endogenously express Moreover, our findings propose a therapeutic potential in combined CXCR4 and LPA1 inhibitors for cancer

University of Utah School of Medicine in Salt Lake City, UT, and an investigator with the Huntsman Cancer focuses on Smoothened and other class F GPCRs which play essential roles in embryonic development and in cancer Ben studied developmental and cancer signaling as a postdoctoral fellow with Philip Beachy at Stanford

the receptor tyrosine kinases family and overexpression of EGFR has been linked to poor prognosis and cancer SSTR2 and EGFR was evaluated by immunohistochemistry (IHC) in 491 cases of NPC and 50 cases of non-cancerous High expression of SSTR2 and EGFR was significantly increased in NPC patients compared with non-cancerous

PDF Program HERE < Back to Full Agenda Posters Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Caroline Formstone Abstract "Breast cancer is the most common form of cancer amongst women. Recent studies identify CELSR1, a key PCP gene, as a novel biomarker for early-stage breast cancer. The impact of CELSR1 on cancer progression, however, is unclear. Notably, our pilot data from luminal-type breast cancer cell lines representative of breast carcinomas

2022 Abstract Due to its high metastatic potential, malignant melanoma is one of the deadliest skin cancers In melanoma as well as in other cancers, acidification of the tumor microenvironment (= TME, inverse