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. 2006 Feb 23;49(4):1227-30.
doi: 10.1021/jm051099t.

1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b

Graeme Semple, Philip J Skinner, Martin C Cherrier, Peter J Webb, Carleton R Sage, Susan Y Tamura, Ruoping Chen, Jeremy G Richman, Daniel T Connolly

1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b

Graeme Semple et al. J Med Chem. .

Abstract

1-Substituted benzotriazole carboxylic acids have been identified as the first reported examples of selective small-molecule agonists of the human orphan G-protein-coupled receptor GPR109b (HM74), a low-affinity receptor for the HDL-raising drug niacin. No activity was observed at the highly homologous high-affinity niacin receptor GPR109a (HM74A). The high degree of selectivity was attributed to a difference in the amino acid sequence adjacent to a key arginine-ligand interaction allowing somewhat larger ligands to be tolerated by GPR109b.

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