ADRA1A
ADRA1A (Alpha-1A adrenergic receptor) is a receptor that reads hormone signals inside the cell nucleus. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Neuroendocrine tumours and Prostate cancer.
Overview
Alpha-1 adrenergic receptors are G protein-coupled receptors for catecholamines that signal through the G(q) family of G proteins, including G(q) and G(11). Upon activation, they stimulate the phosphatidylinositol-calcium second messenger pathway, leading to calcium release from intracellular stores and activation of protein kinase C. ADRA1A binds the catecholamine ligands norepinephrine and epinephrine.
Open Targets scores its association with cancer at 0.58 (direct and indirect evidence; datatypes literature 0.40, genetic association 0.29, clinical 0.86).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · ADRA1A (Alpha-1A adrenergic receptor) is a receptor that reads hormone signals inside the cell nucleus. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Neuroendocrine tumours and Prostate cancer.
- 1 · What it is
ADRA1A (Alpha-1A adrenergic receptor) is a receptor that reads hormone signals inside the cell nucleus. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Neuroendocrine tumours and Prostate cancer.
- 2 · What goes wrong in cancer
Alpha-1 adrenergic receptors are G protein-coupled receptors for catecholamines that signal through the G(q) family of G proteins, including G(q) and G(11).
- 3 · How drugs use it
No product in this corpus aims at ADRA1A yet. Drugs cut off the hormone supply, block the receptor so the hormone cannot bind, or send the receptor to the cell's waste disposal.
External identifiers
Sources: HGNC HGNC:277 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P35348 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000120907 (association with cancer (MONDO_0004992) 0.58; per-cancer scores at or above 0.5: prostate cancer 0.50, neuroendocrine neoplasm 0.51 (GraphQL API, CC0))
Biology
Alpha-1 adrenergic receptors are G protein-coupled receptors for catecholamines that signal through the G(q) family of G proteins, including G(q) and G(11). Upon activation, they stimulate the phosphatidylinositol-calcium second messenger pathway, leading to calcium release from intracellular stores and activation of protein kinase C. ADRA1A binds the catecholamine ligands norepinephrine and epinephrine. Can also couple to G(14) protein. Nuclear ADRA1A forms heterooligomers with ADRA1B to regulate phenylephrine(PE)-stimulated ERK signalling in cardiac myocytes. At the plasma membrane, ADRA1A interacts with CAVIN4/MURC to regulates ERK activation in cardiomyocytes, contributing to the regulation of cardiac hypertrophy. Location: Nucleus membrane; Cell membrane; Cytoplasm; Membrane, caveola (UniProt). Locus 8p21.2 (HGNC).
- Neuroendocrine tumours: Open Targets association 0.51 with neuroendocrine neoplasm (MONDO_0019496)
- Prostate cancer: Open Targets association 0.50 with prostate cancer (MONDO_0008315)
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 0.86. 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:"ADRA1A" OR ABSTRACT:"ADRA1A" OR TITLE:"adrenoceptor alpha 1A" OR ABSTRACT:"adrenoceptor alpha 1A" OR TITLE:"Alpha-1A adrenergic receptor" OR ABSTRACT:"Alpha-1A adrenergic receptor" OR TITLE:"ADRA1L1" OR ABSTRACT:"ADRA1L1" OR TITLE:"ADRA1C" OR ABSTRACT:"ADRA1C") 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 ADRA1A, not a curated reading list.