Introduction of HCAR3
HCAR3 (Hydroxycarboxylic acid receptor 3), also known as niacin receptor 2 (NIACR2), GPR109B and GPRHM74, is encoded by HCAR3 gene. It is a Gi/Go-coupled G protein-coupled receptor which belongs to the hydroxycarboxylic acid family (the other identified member being HCA2). This receptor is predominantly expressed in adipocytes and mediates antilipolytic effects. The ligands of HCAR3 have been identified as 3-hydroxylated b-oxidation intermediates, in particular 3-hydroxy-octanoate. HCAR3 also has low-affinity binding with nicotinic acid (niacin).
|Basic Information ofHCAR3|
|Protein Name||Hydroxycarboxylic acid receptor 3|
|Aliases||GPR109B, GPRHM74,NIACR2, Nicotinic acid receptor 2|
|Organism||Homo sapiens (Human)|
Function of HCAR3 Membrane Protein
The binding of nicotinic acid to HCAR3 leads to a G-protein-mediated decrease in cAMP levels. 3-OH-octanoic acid has anti-lipolytic activity, and its plasma concentration in humans reflects the β-oxidation flux, and it is a highly specific agonist of HCAR3. Studies have shown that HCAR3 and 3-OH-octanoic acid also mediate a negative feedback regulation of adipocyte lipolysis to offset prolipolytic impacts on the conditions that the β-oxidation rates increase physiologically or pathologically. This pharmacological effect calls for much higher nicotinic acid doses compared with those provided by a normal diet. HCAR3 is shown to inhibit forskolin-induced activation of a cAMP response element through the D isomers of tryptophan, phenylalanine, and kynurenic acid. Given the wide expression of HCAR3 in various immune and inflammatory cells, it will undoubtedly be interesting to investigate the potential of HCAR3 agonists to treat immune disorders of the skin but also of other organs.
Fig.1 Structure of G protein-coupled receptors membrane protein.
Application of HCAR3 Membrane Protein in Literature
This article suggested that the aromatic D-amino acids, such as D-phenylalanine and D-tryptophan, elicited a chemotactic response in human neutrophils via activation of GPR109B.
The results of this article indicated that the ligand-receptor pair 3-OH-octanoic acid/GPR109B in humans mediated a negative feedback regulation of adipocyte lipolysis to counteract prolipolytic influences under conditions of physiological or pathological increases in beta-oxidation rates.
Authors in this group demonstrated that HM74 and HM74a can mediate macrophage responses to niacin via activation of the prostaglandin synthesis pathway and induction and activation of PPARgamma. This suggested a novel mechanism(s) mediating the clinical effects of pharmacological doses of niacin.
This article proposes that the hydroxy-carboxylic acid structure of their endogenous ligands was the defining property of this receptor subfamily and that hydroxy-carboxylic acid receptors functioned as metabolic sensors which fine-tune the regulation of metabolic pathways.
HCAR3 Preparation Options
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