Source:http://linkedlifedata.com/resource/pubmed/id/17070058
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2006-11-20
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pubmed:abstractText |
We report here the design and parallel synthesis of 217 compounds based on a malonic-hydroxamic acid template. These compounds are obtained via a two-step solution-phase procedure. The set of diverse building-blocks used makes this strategy suitable for the search of inhibitors of various metallo-proteases and for the investigation of the biological role of new metallo-proteases. As a proof of concept, we screened this library on Neutral Aminopeptidase (APN; EC 3.4.11.2), the prototypal enzyme of the M1 family. Several submicromolar inhibitors were identified.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0968-0896
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
63-76
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pubmed:meshHeading |
pubmed-meshheading:17070058-Aminopeptidases,
pubmed-meshheading:17070058-Animals,
pubmed-meshheading:17070058-Combinatorial Chemistry Techniques,
pubmed-meshheading:17070058-Drug Design,
pubmed-meshheading:17070058-Drug Evaluation, Preclinical,
pubmed-meshheading:17070058-Enzyme Activation,
pubmed-meshheading:17070058-Hydroxamic Acids,
pubmed-meshheading:17070058-Kidney,
pubmed-meshheading:17070058-Microsomes,
pubmed-meshheading:17070058-Molecular Structure,
pubmed-meshheading:17070058-Protease Inhibitors,
pubmed-meshheading:17070058-Stereoisomerism,
pubmed-meshheading:17070058-Structure-Activity Relationship,
pubmed-meshheading:17070058-Swine,
pubmed-meshheading:17070058-Zinc
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pubmed:year |
2007
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pubmed:articleTitle |
A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening.
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pubmed:affiliation |
Inserm, U761, University of Lille 2, Faculty of Pharmacy, Institut Pasteur Lille, "Biostructures and Drug Discovery" 3 rue du Pr Laguesse F-59006 Lille cedex, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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