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Target intelligence / Profile preview
Hydroxycarboxylic acid receptor 2 (HCAR2)
- Target
- HCAR2
- Molecular classification
- G protein-coupled receptor, GPCR, Class A GPCR
01
Overview
Hydroxycarboxylic acid receptor 2 (HCAR2), also known as GPR109A or NIACR1, is a G protein-coupled receptor that primarily couples to Gi/o proteins. Endogenous ligands include β-hydroxybutyrate and butyrate. HCAR2 activation inhibits lipolysis, modulates inflammation, and regulates neutrophil apoptosis. It is a validated drug target for dyslipidemia and a potential target for inflammatory and neurodegenerative diseases.
- Other names
- GPR109AHCA2HM74aHM74bNIACR1PUMAGPuma-gNiacin receptor 1
02
Mechanism of action
Activation of HCAR2 primarily couples to Gi/o proteins upon ligand binding, leading to inhibition of adenylate cyclase activity and decreased intracellular cAMP levels. Promotes production and release of prostaglandins like PGD₂ and PGE₂ via arachidonic acid pathway activation.
03
Biological functions
Inhibition of lipolysisModulation of inflammationRegulation of neutrophil apoptosisSignal transduction
04
Disease associations
DyslipidemiaHyperlipidemiaInflammatory diseasesNeurodegenerative diseasesAlzheimer’s diseaseParkinson’s disease
05
Safety considerations
Cutaneous flushing during niacin therapy
06
Interacting drugs
Niacin
5 more in the full profile.
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