Tclin ADRA2A Alpha-2A adrenergic receptor

Protein Summary

Description

Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor 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. Alpha-2-adrenergic receptors are members of the G protein-coupled receptor superfamily. They include 3 highly homologous subtypes: alpha2A, alpha2B, and alpha2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. Studies in mouse revealed that both the alpha2A and alpha2C subtypes were required for normal presynaptic control of transmitter release from sympathetic nerves in the heart and from central noradrenergic neurons; the alpha2A subtype inhibited transmitter release at high stimulation frequencies, whereas the alpha2C subtype modulated neurotransmission at lower levels of nerve activity. This gene encodes alpha2A subtype and it contains no introns in either its coding or untranslated sequences. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P08913
• B0LPF6
• Q2I8G2
• Q2XN99
• Q86TH8
• Q9BZK1

Gene Name

• ADRA2A

Ensembl ID

• ENST00000280155
• ENSP00000280155
• ENSG00000150594

Symbol

• ADRA2R
• ADRAR
• ADRA2
• ADRAR
• ZNF32
• ADRA2R
• ALPHA2AAR

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
drug	1
molecular function	0.96
ligand (chemical)	0.94
PubMedID	0.93

Protein Classes

PANTHER Classes

Protein / Receptor / G-protein Coupled Receptor / Alpha-2a Adrenergic Receptor

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Adrenoceptor / Alpha Adrenoceptor / Alpha-2a Adrenergic Receptor

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 401.63   (req: < 5)

Gene RIFs: 142   (req: <= 3)

Antibodies: 292   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 401.63   (req: >= 5)

Gene RIFs: 142   (req: > 3)

Antibodies: 292   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 49

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 351

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 46