Loading
GPR65 is a sensor on immune cells that detects acidity. Tumours are often acidic, and the idea behind blocking GPR65 is to stop that acidity from turning nearby immune cells into ones that help the tumour; a GPR65 inhibitor is in an early trial.
GPR65 (chromosome 14q31.3) is a proton-sensing G protein-coupled receptor activated by extracellular pH, mainly coupled to G(s) and adenylate cyclase (UniProt Q8IYL9); it is expressed predominantly in immune cells (doi:10.1016/j.bbadis.2021.166288). A 2013 review in Frontiers in Physiology describes the tumour microenvironment as acidic because of glycolytic metabolism, hypoxia and poor perfusion, and the pH-sensing receptors GPR4, GPR65, GPR68 and GPR132 as regulators of cancer cell spread, immune cell function, inflammation and blood vessel formation (Justus et al., doi:10.3389/fphys.2013.00354). In OnCo, PTT-4256 is an oral GPR65 inhibitor; its developer's case is that tumour acidity acts through GPR65 to switch immune cells into a suppressed, pro-tumour state.
In plain words · GPR65 is a sensor on immune cells that detects acidity. Tumours are often acidic, and the idea behind blocking GPR65 is to stop that acidity from turning nearby immune cells into ones that help the tumour; a GPR65 inhibitor is in an early trial.
GPR65 is a sensor on immune cells that detects acidity. Tumours are often acidic, and the idea behind blocking GPR65 is to stop that acidity from turning nearby immune cells into ones that help the tumour; a GPR65 inhibitor is in an early trial.
Proton-sensing receptor (also called TDAG8) that signals through G(s) and cyclic AMP; it may also bind the glycosphingolipid psychosine (UniProt Q8IYL9).
1 product aims at GPR65: small molecules. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
Proton-sensing receptor (also called TDAG8) that signals through G(s) and cyclic AMP; it may also bind the glycosphingolipid psychosine (UniProt Q8IYL9).
PTT-4256 is an experimental oral small molecule from Pathios Therapeutics, in phase 1 trials for advanced solid tumours.
Query for this target: (TITLE:"GPR65" OR ABSTRACT:"GPR65" OR TITLE:"G protein-coupled receptor 65" OR ABSTRACT:"G protein-coupled receptor 65" OR TITLE:"TDAG8" OR ABSTRACT:"TDAG8") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about GPR65, not a curated reading list.
Shares Metastatic cancer (cancer that has spread) and the tag pipeline-gap-target.
Shares Metastatic cancer (cancer that has spread) and the tag pipeline-gap-target.
Shares Metastatic cancer (cancer that has spread) and the tag pipeline-gap-target.
Shares Metastatic cancer (cancer that has spread) and the tag pipeline-gap-target.
Shares PTT-4256, Metastatic cancer (cancer that has spread).
Every source this page cites, grouped by who published it. Grouping is read from the web address, not assigned by hand.
A source that has moved or gone is reported by the weekly link check. /audit/