2. Academic Validation
  3. 1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b

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

  • J Med Chem. 2006 Feb 23;49(4):1227-30. doi: 10.1021/jm051099t.
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
PMID: 16480258 DOI: 10.1021/jm051099t
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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