Tclin HTR2A 5-hydroxytryptamine receptor 2A

Protein Summary

Description

G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:1330647, PubMed:18703043, PubMed:19057895). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD) (PubMed:28129538). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors (PubMed:28129538). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:28129538). Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores (PubMed:18703043, PubMed:28129538). Affects neural activity, perception, cognition and mood (PubMed:18297054). Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction. (Microbial infection) Acts as a receptor for human JC polyomavirus/JCPyV. This gene encodes one of the receptors for serotonin, a neurotransmitter with many roles. Mutations in this gene are associated with susceptibility to schizophrenia and obsessive-compulsive disorder, and are also associated with response to the antidepressant citalopram in patients with major depressive disorder (MDD). MDD patients who also have a mutation in intron 2 of this gene show a significantly reduced response to citalopram as this antidepressant downregulates expression of this gene. Multiple transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Sep 2009]

Uniprot Accession IDs

• P28223
• B2RAC5
• B4DZ79
• F5GWE8
• Q5T8C0
• 5-HT-2

Gene Name

• HTR2A

Ensembl ID

• ENST00000378688
• ENSP00000367959
• ENSG00000102468
• ENST00000542664
• ENSP00000437737
• ENST00000543956
• ENSP00000441861

Symbol

• HTR2
• HTR2
• 5-HT2A

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
drug	1
ligand (chemical)	1
chemical	0.9
kinase perturbation	0.81

Protein Classes

PANTHER Classes

Protein / Receptor / G-protein Coupled Receptor / 5-hydroxytryptamine Receptor 2a

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / 5-hydroxytryptamine Receptor / 5-ht2 Receptor / 5-hydroxytryptamine Receptor 2a

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: 2969.43   (req: < 5)

Gene RIFs: 488   (req: <= 3)

Antibodies: 325   (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: 2969.43   (req: >= 5)

Gene RIFs: 488   (req: > 3)

Antibodies: 325   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 43

Tchem

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

Active Ligands: 2583

Tclin

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

Active Drugs: 82