ADRA2A
ADRA2A (Alpha-2A adrenergic 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 Neuroendocrine tumours.
Overview
Alpha-2 adrenergic receptors are G protein-coupled receptors for catecholamines that activate the G(i/o) protein pathway, thereby promoting adenylyl cyclase inhibition, ERK1/2 stimulation, and voltage-gated calcium channels suppression. Control a variety of physiological processes, such as regulation of blood pressure, lipolysis and insulin release. ADRA2A and ADRA2C mediates the presynaptic feedback inhibition of neurotransmitter release from noradrenergic nerve terminals in sympathetic and central nervous systems.
Open Targets scores its association with cancer at 0.52 (direct and indirect evidence; datatypes literature 0.89, clinical 0.81).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · ADRA2A (Alpha-2A adrenergic 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 Neuroendocrine tumours.
- 1 · What it is
ADRA2A (Alpha-2A adrenergic 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 Neuroendocrine tumours.
- 2 · What goes wrong in cancer
Alpha-2 adrenergic receptors are G protein-coupled receptors for catecholamines that activate the G(i/o) protein pathway, thereby promoting adenylyl cyclase inhibition, ERK1/2 stimulation, and voltage-gated calcium channels suppression.
- 3 · How drugs use it
No product in this corpus aims at ADRA2A 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:281 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P08913 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000150594 (association with cancer (MONDO_0004992) 0.52; per-cancer scores at or above 0.5: neuroendocrine neoplasm 0.51 (GraphQL API, CC0))
Biology
Alpha-2 adrenergic receptors are G protein-coupled receptors for catecholamines that activate the G(i/o) protein pathway, thereby promoting adenylyl cyclase inhibition, ERK1/2 stimulation, and voltage-gated calcium channels suppression. Control a variety of physiological processes, such as regulation of blood pressure, lipolysis and insulin release. ADRA2A and ADRA2C mediates the presynaptic feedback inhibition of neurotransmitter release from noradrenergic nerve terminals in sympathetic and central nervous systems. ADRA2A inhibits transmitter release at high stimulation frequencies, whereas ADRA2C modulates neurotransmission at lower levels of nerve activity. The rank order of potency for agonists of ADRA2A is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol. Location: Cell membrane (UniProt). Locus 10q25.2 (HGNC).
- Neuroendocrine tumours: Open Targets association 0.51 with neuroendocrine neoplasm (MONDO_0019496)
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 0.81. 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:"ADRA2A" OR ABSTRACT:"ADRA2A" OR TITLE:"adrenoceptor alpha 2A" OR ABSTRACT:"adrenoceptor alpha 2A" OR TITLE:"Alpha-2A adrenergic receptor" OR ABSTRACT:"Alpha-2A adrenergic receptor" OR TITLE:"ADRAR" OR ABSTRACT:"ADRAR" OR TITLE:"ADRA2" OR ABSTRACT:"ADRA2" OR TITLE:"ADRA2R" OR ABSTRACT:"ADRA2R") 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 ADRA2A, not a curated reading list.