Tclin HCAR2 Hydroxycarboxylic acid receptor 2

Protein Summary

Description

Acts as a high affinity receptor for both nicotinic acid (also known as niacin) and (D)-beta-hydroxybutyrate and mediates increased adiponectin secretion and decreased lipolysis through G(i)-protein-mediated inhibition of adenylyl cyclase. This pharmacological effect requires nicotinic acid doses that are much higher than those provided by a normal diet. Mediates nicotinic acid-induced apoptosis in mature neutrophils. Receptor activation by nicotinic acid results in reduced cAMP levels which may affect activity of cAMP-dependent protein kinase A and phosphorylation of target proteins, leading to neutrophil apoptosis. The rank order of potency for the displacement of nicotinic acid binding is 5-methyl pyrazole-3-carboxylic acid = pyridine-3-acetic acid > acifran > 5-methyl nicotinic acid = acipimox >> nicotinuric acid = nicotinamide.

Uniprot Accession IDs

• Q8TDS4
• A0PJL5
• A7LGG3

Gene Name

• HCAR2

Ensembl ID

• ENST00000328880
• ENSP00000375066
• ENSG00000182782

Symbol

• GPR109A
• HCA2
• HM74A
• NIACR1
• HCA2
• HM74a
• HM74b
• PUMAG
• NIACR1
• Puma-g
• GPR109A

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
ligand (chemical)	0.76
chemical	0.63
cell line	0.62
biological process	0.57
biological term	0.51

Protein Classes

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Hydroxycarboxylic Acid Receptor / Hydroxycarboxylic Acid Receptor 2

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: 267.12   (req: < 5)

Gene RIFs: 44   (req: <= 3)

Antibodies: 188   (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: 267.12   (req: >= 5)

Gene RIFs: 44   (req: > 3)

Antibodies: 188   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 6

Tchem

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

Active Ligands: 204

Tclin

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

Active Drugs: 2