Tclin HTR2C 5-hydroxytryptamine receptor 2C

Protein Summary

Description

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis. This gene encodes a seven-transmembrane G-protein-coupled receptor. The encoded protein responds to signaling through the neurotransmitter serotonin. The mRNA of this gene is subject to multiple RNA editing events, where adenosine residues encoded by the genome are converted to inosines. RNA editing is predicted to alter the structure of the second intracellular loop, thereby generating alternate protein forms with decreased ability to interact with G proteins. Abnormalities in RNA editing of this gene have been detected in victims of suicide that suffer from depression. In addition, naturally-occuring variation in the promoter and 5' non-coding and coding regions of this gene may show statistically-significant association with mental illness and behavioral disorders. Alternative splicing results in multiple different transcript variants. [provided by RefSeq, Jan 2015]

Uniprot Accession IDs

• P28335
• B1AMW4
• Q5VUF8
• Q9NP28
• 5-HT-2C

Gene Name

• HTR2C

Ensembl ID

• ENST00000276198
• ENSP00000276198
• ENSG00000147246
• ENST00000371950
• ENSP00000361018
• ENST00000371951
• ENSP00000361019

Symbol

• HTR1C
• HTR1C
• 5-HT1C
• 5-HT2C
• 5HTR2C
• 5-HTR2C

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
drug	1
ligand (chemical)	1
biological process	0.97
disease	0.8
phenotype	0.75

Protein Classes

PANTHER Classes

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

DTO Classes

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

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: 1237.95   (req: < 5)

Gene RIFs: 175   (req: <= 3)

Antibodies: 456   (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: 1237.95   (req: >= 5)

Gene RIFs: 175   (req: > 3)

Antibodies: 456   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 27

Tchem

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

Active Ligands: 1524

Tclin

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

Active Drugs: 52