Recently, many novel discoveries have underlined the regulatory roles of neurotransmitters in the microenvironment of the most novel advances concerning the role of neurotransmitters in the normal neural and the GBM microenvironments

August 2022 "The common mechanisms by which members of the G protein-coupled receptor (GPCR) family respond to neurotransmitters in the brain have been well studied. However, it is becoming increasingly clear that GPCRs show great diversity in their intracellular location, interacting partners and effectors, and signaling consequences. Here we will discuss recent studies on the diversity of location, effectors, and signaling of GPCRs, and how these could interact to generate specific spatiotemporal patterns of GPCR signaling in cells." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent GPCR ligands "G-protein coupled receptors (GPCRs) have been largely targeted in a wide range of diseases, but few therapies have been directed against GPCRs in the field of cancer, partly because of the lack of effective target identification strategies. Here, using colorectal cancer (CRC) as a model, we explored the gene expression of a panel of GPCRs in tumor and stromal cells, identifying specific gene sets defining each cellular compartment. We selected the adenosine receptor 2B (A2BAR), specifically expressed in cancer cell lines compared with stromal cells, to explore the use of fluorescent ligands that can be used for target visualization. Fluorescent probes allowed semi-quantitative receptor mapping in living cells and validated the specific expression of A2BAR in CRC cell lines. As well, fluorescent ligands were effective at monitoring real-time A2BAR receptor labeling using live-imaging modalities, and displayed high efficiency when used to label complex 3D cellular systems such as tumor spheroids. Finally, we validated A2BAR as a potential pharmacological tool in CRC, using selective antagonists, finding a reduction in tumor cell proliferation. This proof-of-concept study suggests the use of fluorescent ligands for GPCR characterization through imaging, and as possible new tools used for target validation in drug screening methodologies." Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR News < GPCRs in Oncology and Immunology GPCR signaling contributes to immune characteristics of microenvironment Single-cell transcriptome further delineated the tumor microenvironment as immune-inflamed, -deficient chemokine receptor-1 (CCR1) on malignant and immunosuppressive cells modulated virus-cancer interaction on microenvironment , Li Wang , Peng-Peng Xu , Sai-Juan Chen , Wei-Li Zhao Tags CCR1 , Epstein-Barr virus , Lymphoma , Microenvironment

< GPCR News < GPCRs in Oncology and Immunology Metabolic crosstalk: Extracellular ATP and the tumor microenvironment In the tumor microenvironment (TME), purinergic receptors such as ATP-gated ion channels P2X1-5 and G ) , Immunosuppression , Purinergic receptors , Purinergic signaling , Therapeutic potential , Tumor microenvironment

News < GPCRs in Oncology and Immunology RGS5 maintaining vascular homeostasis is altered by the tumor microenvironment Conclusions: These findings suggest that tumor microenvironment shifts the function of RGS5 from anti-inflammation