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EDNRA (Endothelin-1 receptor) is a gene. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Prostate cancer.
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3.
Open Targets scores its association with cancer at 0.55 (direct and indirect evidence; datatypes literature 0.94, animal model 0.71, genetic association 0.00, clinical 0.85).
In plain words · EDNRA (Endothelin-1 receptor) is a gene. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Prostate cancer.
EDNRA (Endothelin-1 receptor) is a gene. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Prostate cancer.
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
2 products aim at EDNRA: small molecules. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
Specificity not established: no corpus medicine is aimed at it and the catalogues give it only the role drug-target; HPA finds the RNA tissue enhanced, which says where the protein sits but not whether the tumour differs from normal tissue. HPA EDNRA: RNA tissue enhanced (seminal vesicle 107 nTPM); no normal tissue stained high; highest cancer staining pancreatic cancer (2 of 11 high). Distribution: 1 cancer family in the corpus carries a prevalence row, label threshold or catalogue link for it (Prostate cancer); Open Targets associates it with 1 specific cancer type at or above 0.5 (prostate cancer). (No rule of scripts/fetch-target-specificity.ts fired.)
Sources: Human Protein Atlas EDNRA tissue; Open Targets ENSG00000151617 associations
First described 1991. Earliest sequence paper UniProt cites for the protein: Adachi et al, Biochem. Biophys. Res. Commun, 1991, "Cloning and characterization of cDNA encoding human A-type endothelin receptor". Source.
Sources: HGNC HGNC:3179 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P25101 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000151617 (association with cancer (MONDO_0004992) 0.55; per-cancer scores at or above 0.5: prostate cancer 0.52 (GraphQL API, CC0))
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3. Location: Cell membrane (UniProt). Locus 4q31.22-q31.23 (HGNC).
RNA: tissue enhanced (seminal vesicle 107 nTPM), detected in many normal tissues.
No normal tissue stained high.
Medium only: carcinoid, cervical cancer, colorectal cancer, endometrial cancer.
HPA EDNRA tissue · HPA EDNRA pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
The other endothelin blocker. Adding it to chemotherapy for advanced prostate cancer changed nothing, and the trial was stopped for futility.
A drug blocking a signal that prostate cancer uses to grow in bone. Three trials in prostate cancer found no survival benefit and it was dropped.
Query for this target: (TITLE:"EDNRA" OR ABSTRACT:"EDNRA" OR TITLE:"endothelin receptor type A" OR ABSTRACT:"endothelin receptor type A" OR TITLE:"Endothelin-1 receptor" OR ABSTRACT:"Endothelin-1 receptor" OR TITLE:"ET-A" OR ABSTRACT:"ET-A" OR TITLE:"ETA-R" OR ABSTRACT:"ETA-R" OR TITLE:"hET-AR" OR ABSTRACT:"hET-AR") 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 EDNRA, not a curated reading list.
Shares Zibotentan, Atrasentan, ENTHUSE M1, SWOG S0421.
Shares ENTHUSE M1, SWOG S0421, Prostate cancer.
Shares SWOG S0421, Prostate cancer.
Shares SWOG S0421, Prostate cancer.
Shares Zibotentan, Atrasentan, ENTHUSE M1, SWOG S0421.
Shares Atrasentan, SWOG S0421.