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rdf:type |
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|
lifeskim:mentions |
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pubmed:issue |
13
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pubmed:dateCreated |
2003-6-12
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pubmed:abstractText |
A series of pyridine-2-carboxylic acid derivatives were synthesized according to the leads from the screening, and potent inhibitors have been obtained by structural modification. They have shown submicromolar inhibition of the enzymes (for example, for 9n, IC(50) = 130 nM for EcMetAP1 and IC(50) = 380 nM for ScMetAP1). They represent small-molecule MetAP inhibitors with novel structures different from alkylating fumagillin derivatives and peptidic bestatin-based MetAP inhibitor.
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pubmed:grant |
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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 |
|
|
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:ChenLing-LingLL,
pubmed-author:LiJing-YaJY,
pubmed-author:LiuZhi-YingZY,
pubmed-author:LuoQun-LiQL,
pubmed-author:LushingtonGerald HGH,
pubmed-author:NanFa-JunFJ,
pubmed-author:OsL OLO,
pubmed-author:QianZhenZ,
pubmed-author:ShenQiangQ,
pubmed-author:YeQi-ZhuangQZ,
pubmed-author:YuLiL
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pubmed:issnType |
Print
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pubmed:day |
19
|
|
pubmed:volume |
46
|
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pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
2631-40
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:12801227-Aminopeptidases,
pubmed-meshheading:12801227-Anti-Bacterial Agents,
pubmed-meshheading:12801227-Anti-Infective Agents,
pubmed-meshheading:12801227-Binding Sites,
pubmed-meshheading:12801227-Crystallography, X-Ray,
pubmed-meshheading:12801227-Enzyme Inhibitors,
pubmed-meshheading:12801227-Escherichia coli,
pubmed-meshheading:12801227-Models, Molecular,
pubmed-meshheading:12801227-Protein Binding,
pubmed-meshheading:12801227-Pyridines,
pubmed-meshheading:12801227-Saccharomyces cerevisiae,
pubmed-meshheading:12801227-Structure-Activity Relationship,
pubmed-meshheading:12801227-Thiazoles
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pubmed:year |
2003
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pubmed:articleTitle |
Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae.
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pubmed:affiliation |
Chinese National Center for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Institutes for Life Sciences, Chinese Academy of Sciences, 189 Guo Shou Jing Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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