Identification of a nicotinic acid receptor: is this the molecular target for the oldest lipid-lowering drug?
Nicotinic acid has been used clinically for over 40 years in the treatment of dyslipidemia, producing a desirable normalization of a range of cardiovascular risk factors. The precise mechanism of action of nicotinic acid is unknown, although it is believed that activation of a Gi-type G protein-coupled receptor, resulting in the inhibition of adipocyte lipolysis, may contribute. This review describes the identification of this elusive receptor, and outlines the evidence suggesting that this may be the molecular target for the clinical effects of nicotinic acid.
Pike
Nicholas B
NB
Cardiovascular and Urogenital Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK. nick.b.pike@gsk.com
Wise
Alan
A
D000818:Animals; D016503:Drug Delivery Systems; D005663:Furans / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D000960:Hypolipidemic Agents / Q000737:chemistry / Q000494:pharmacology*; D008024:Ligands; D009525:Niacin / Q000737:chemistry / Q000494:pharmacology*; D043562:Receptors, G-Protein-Coupled; D011978:Receptors, Nicotinic / Q000187:drug effects* / Q000378:metabolism
D005663:Furans; C473653:HCAR3 protein, human; D000960:Hypolipidemic Agents; D008024:Ligands; D043562:Receptors, G-Protein-Coupled; D011978:Receptors, Nicotinic; D009525:Niacin; C036804:acifran