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

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 homolog... Full description

Journal Title: Journal of medicinal chemistry 23 February 2006, Vol.49(4), pp.1227-30
Main Author: Semple, Graeme
Other Authors: Skinner, Philip J , Cherrier, Martin C , Webb, Peter J , Sage, Carleton R , Tamura, Susan Y , Chen, Ruoping , Richman, Jeremy G , Connolly, Daniel T
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: ISSN: 0022-2623 ; PMID: 16480258 Version:1
Link: http://pubmed.gov/16480258
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recordid: medline16480258
title: 1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b
format: Article
creator:
  • Semple, Graeme
  • Skinner, Philip J
  • Cherrier, Martin C
  • Webb, Peter J
  • Sage, Carleton R
  • Tamura, Susan Y
  • Chen, Ruoping
  • Richman, Jeremy G
  • Connolly, Daniel T
subjects:
  • Carboxylic Acids -- Chemical Synthesis
  • Hypolipidemic Agents -- Chemical Synthesis
  • Receptors, G-Protein-Coupled -- Agonists
  • Triazoles -- Chemical Synthesis
ispartof: Journal of medicinal chemistry, 23 February 2006, Vol.49(4), pp.1227-30
description: 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.
language: eng
source:
identifier: ISSN: 0022-2623 ; PMID: 16480258 Version:1
fulltext: fulltext
issn:
  • 00222623
  • 0022-2623
url: Link


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title1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b
creatorSemple, Graeme ; Skinner, Philip J ; Cherrier, Martin C ; Webb, Peter J ; Sage, Carleton R ; Tamura, Susan Y ; Chen, Ruoping ; Richman, Jeremy G ; Connolly, Daniel T
ispartofJournal of medicinal chemistry, 23 February 2006, Vol.49(4), pp.1227-30
identifierISSN: 0022-2623 ; PMID: 16480258 Version:1
subjectCarboxylic Acids -- Chemical Synthesis ; Hypolipidemic Agents -- Chemical Synthesis ; Receptors, G-Protein-Coupled -- Agonists ; Triazoles -- Chemical Synthesis
description1-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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abstract1-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.
pmid16480258
doi10.1021/jm051099t
eissn15204804
date2006-02-23