CASR
CASR (Extracellular calcium-sensing receptor) is a gene. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it.
Overview
G protein-coupled receptor that senses changes in the extracellular concentration of calcium ions and plays a key role in maintaining calcium homeostasis. Senses fluctuations in the circulating calcium concentration: activated by elevated circulating calcium, leading to decreased parathyroid hormone (PTH) secretion in parathyroid glands. In kidneys, acts as a key regulator of renal tubular calcium resorption.
Open Targets scores its association with cancer at 0.61 (direct and indirect evidence; datatypes clinical 0.91, literature 0.98, genetic association 0.00, somatic mutation 0.23, animal model 0.59).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · CASR (Extracellular calcium-sensing receptor) is a gene. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it.
- 1 · What it is
CASR (Extracellular calcium-sensing receptor) is a gene. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it.
- 2 · What goes wrong in cancer
G protein-coupled receptor that senses changes in the extracellular concentration of calcium ions and plays a key role in maintaining calcium homeostasis.
- 3 · How drugs use it
No product in this corpus aims at CASR yet. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
External identifiers
Sources: HGNC HGNC:1514 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P41180 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000036828 (association with cancer (MONDO_0004992) 0.61; (GraphQL API, CC0))
Biology
G protein-coupled receptor that senses changes in the extracellular concentration of calcium ions and plays a key role in maintaining calcium homeostasis. Senses fluctuations in the circulating calcium concentration: activated by elevated circulating calcium, leading to decreased parathyroid hormone (PTH) secretion in parathyroid glands. In kidneys, acts as a key regulator of renal tubular calcium resorption. Ligand binding causes a conformation change that triggers signalling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. CASR is coupled with different G(q)/G(11), G(i)/G(o)- or G(s)-classes of G proteins depending on the context. In the parathyroid and kidney, CASR signals through G(q)/G(11) and G(i)/G(o) G proteins: G(q)/G(11) coupling activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers, while G(i)/G(o) coupling mediates inhibition of adenylate cyclase activity. Location: Cell membrane (UniProt). Locus 3q13.33-q21.1 (HGNC).
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: Open Targets known-drug datatype score 0.91. Evidence tier "approved-drug" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery for this target: (TITLE:"CASR" OR ABSTRACT:"CASR" OR TITLE:"calcium sensing receptor" OR ABSTRACT:"calcium sensing receptor" OR TITLE:"Extracellular calcium-sensing receptor" OR ABSTRACT:"Extracellular calcium-sensing receptor" OR TITLE:"NSHPT" OR ABSTRACT:"NSHPT" OR TITLE:"GPRC2A" OR ABSTRACT:"GPRC2A" OR TITLE:"HHC1" OR ABSTRACT:"HHC1") 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 CASR, not a curated reading list.