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rdf:type |
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lifeskim:mentions |
umls-concept:C0028822,
umls-concept:C0060091,
umls-concept:C0205314,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243077,
umls-concept:C0456387,
umls-concept:C0522095,
umls-concept:C0679622,
umls-concept:C1423759,
umls-concept:C1883254
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pubmed:issue |
14
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pubmed:dateCreated |
2009-7-16
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pubmed:abstractText |
Long chain fatty acid elongase 6 (ELOVL6) catalyzes the elongation of long chain fatty acyl-CoAs and is a potential target for the treatment of metabolic disorders. The ultrahigh throughput screen of our corporate chemical collections resulted in the identification of a novel 3-sulfonyl-8-azabicyclo[3.2.1]octane class of ELOVL6 inhibitor 1a. Optimization of lead 1a led to the identification of the potent, selective, and orally available ELOVL6 inhibitor 1w.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:AraganeKatsumiK,
pubmed-author:KanesakaMakiM,
pubmed-author:KitazawaHidefumiH,
pubmed-author:MiyamotoYasuhisaY,
pubmed-author:NagaseTsuyoshiT,
pubmed-author:NagumoAkiraA,
pubmed-author:SasakiTakahideT,
pubmed-author:SatoNagaakiN,
pubmed-author:ShimamuraKenK,
pubmed-author:TakahashiToshiyukiT,
pubmed-author:TokitaShigeruS,
pubmed-author:YoshimotoRyoR
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pubmed:issnType |
Electronic
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pubmed:day |
23
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4111-4
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pubmed:meshHeading |
pubmed-meshheading:19522500-Acetyltransferases,
pubmed-meshheading:19522500-Animals,
pubmed-meshheading:19522500-Cell Line,
pubmed-meshheading:19522500-Drug Design,
pubmed-meshheading:19522500-Enzyme Inhibitors,
pubmed-meshheading:19522500-Hepatocytes,
pubmed-meshheading:19522500-Humans,
pubmed-meshheading:19522500-Inhibitory Concentration 50,
pubmed-meshheading:19522500-Liver,
pubmed-meshheading:19522500-Male,
pubmed-meshheading:19522500-Mice,
pubmed-meshheading:19522500-Octanes,
pubmed-meshheading:19522500-Rats,
pubmed-meshheading:19522500-Structure-Activity Relationship,
pubmed-meshheading:19522500-Sulfones,
pubmed-meshheading:19522500-Tropanes
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pubmed:year |
2009
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pubmed:articleTitle |
Synthesis and biological evaluation of a novel 3-sulfonyl-8-azabicyclo[3.2.1]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
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pubmed:affiliation |
Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co, Ltd, Tsukuba, Ibaraki 300-2611, Japan. tsnagase@gmail.com
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pubmed:publicationType |
Journal Article
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