rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
4
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pubmed:dateCreated |
2006-2-16
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pubmed:abstractText |
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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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Carboxylic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/HCAR2 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/HCAR3 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Hypolipidemic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Niacin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, G-Protein-Coupled,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Nicotinic,
http://linkedlifedata.com/resource/pubmed/chemical/Triazoles
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-2623
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pubmed:author |
|
pubmed:issnType |
Print
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pubmed:day |
23
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pubmed:volume |
49
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1227-30
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pubmed:dateRevised |
2011-11-3
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pubmed:meshHeading |
pubmed-meshheading:16480258-Adipocytes,
pubmed-meshheading:16480258-Binding Sites,
pubmed-meshheading:16480258-Carboxylic Acids,
pubmed-meshheading:16480258-Cyclic AMP,
pubmed-meshheading:16480258-Humans,
pubmed-meshheading:16480258-Hypolipidemic Agents,
pubmed-meshheading:16480258-Ligands,
pubmed-meshheading:16480258-Lipolysis,
pubmed-meshheading:16480258-Niacin,
pubmed-meshheading:16480258-Receptors, G-Protein-Coupled,
pubmed-meshheading:16480258-Receptors, Nicotinic,
pubmed-meshheading:16480258-Structure-Activity Relationship,
pubmed-meshheading:16480258-Triazoles
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pubmed:year |
2006
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pubmed:articleTitle |
1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b.
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pubmed:publicationType |
Journal Article
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