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Target intelligence / Profile preview
Nicotinic acid receptor 1 (GPR109A)
- Target
- GPR109A
- Molecular classification
- G protein-coupled receptor (GPCR), Receptor
01
Overview
Nicotinic acid receptor 1 (GPR109A/HM74A) is a G protein-coupled receptor highly expressed in adipocytes, macrophages, and other tissues. Activation by niacin and related drugs leads to potent inhibition of fat breakdown (antilipolysis) via Gi/o protein signaling. Its principal therapeutic application is in the correction of lipid disorders, particularly to lower LDL cholesterol and triglycerides, and raise HDL cholesterol, thereby reducing cardiovascular risk. The most prominent adverse effect of targeting GPR109A is cutaneous flushing, resulting from prostaglandin-mediated vasodilation. Research also implicates GPR109A in the modulation of immune function and inflammation through effects in macrophages
- Other names
- Niacin receptor 1HM74APUMA-GNic1GPR109AHydroxycarboxylic acid receptor 2 (HCAR2)
02
Mechanism of action
Agonists (niacin, acipimox) bind GPR109A, trigger Gi/o signaling, decrease cAMP levels, and inhibit lipolysis in adipocytes
03
Biological functions
Signal transduction (inhibitory Gi/o protein pathway)Lipid metabolism regulation (antilipolytic effect in adipocytes)Modulation of immune response (in macrophages)
04
Disease associations
Cardiovascular disease (therapeutic target for lipid lowering)Inflammation (modulation by receptor agonists)Possible roles in dyslipidemia and metabolic syndrome
05
Safety considerations
Cutaneous flushingGlucose intolerancePossible association with insulin resistance
06
Interacting drugs
Nicotinic acid (Niacin)
3 more in the full profile.
07
Biomarkers
No universally accepted clinical biomarkers specific for GPR109A patient selection. HDL/LDL cholesterol, triglycerides, and niacin-induced flushing are surrogate indicators.
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