1-Alkyl-benzotriazole-5-carboxylic Acids Are Highly Selective Agonists of the Human Orphan G-Protein-Coupled Receptor GPR109b
Journal of Medicinal Chemistry2006Vol. 49(4), pp. 1227–1230
Citations Over TimeTop 10% of 2006 papers
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
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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