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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.JM

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.

Authors

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Pub Type(s)

Journal Article

Language

eng

PubMed ID

16480258

Citation

Semple, Graeme, et al. "1-Alkyl-benzotriazole-5-carboxylic Acids Are Highly Selective Agonists of the Human Orphan G-protein-coupled Receptor GPR109b." Journal of Medicinal Chemistry, vol. 49, no. 4, 2006, pp. 1227-30.
Semple G, Skinner PJ, Cherrier MC, et al. 1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b. J Med Chem. 2006;49(4):1227-30.
Semple, G., Skinner, P. J., Cherrier, M. C., Webb, P. J., Sage, C. R., Tamura, S. Y., Chen, R., Richman, J. G., & Connolly, D. T. (2006). 1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b. Journal of Medicinal Chemistry, 49(4), 1227-30.
Semple G, et al. 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. PubMed PMID: 16480258.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b. AU - Semple,Graeme, AU - Skinner,Philip J, AU - Cherrier,Martin C, AU - Webb,Peter J, AU - Sage,Carleton R, AU - Tamura,Susan Y, AU - Chen,Ruoping, AU - Richman,Jeremy G, AU - Connolly,Daniel T, PY - 2006/2/17/pubmed PY - 2006/4/11/medline PY - 2006/2/17/entrez SP - 1227 EP - 30 JF - Journal of medicinal chemistry JO - J Med Chem VL - 49 IS - 4 N2 - 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. SN - 0022-2623 UR - https://www.unboundmedicine.com/medline/citation/16480258/1_Alkyl_benzotriazole_5_carboxylic_acids_are_highly_selective_agonists_of_the_human_orphan_G_protein_coupled_receptor_GPR109b_ L2 - https://doi.org/10.1021/jm051099t DB - PRIME DP - Unbound Medicine ER -