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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
2008-7-21
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pubmed:abstractText |
We demonstrate a fragment-based lead discovery method that combines site-directed ligand discovery with dynamic combinatorial chemistry. Our technique targets dynamic combinatorial screening to a specified region of a protein by using reversible disulfide chemistry. We have used this technology to rapidly identify inhibitors of the drug target Aurora A that span the purine-binding site and the adaptive pocket of the kinase. The binding mode of a noncovalent inhibitor has been further characterized through crystallography.
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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 |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3978-81
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pubmed:dateRevised |
2011-7-11
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pubmed:meshHeading |
pubmed-meshheading:18579375-Binding Sites,
pubmed-meshheading:18579375-Chemistry, Pharmaceutical,
pubmed-meshheading:18579375-Combinatorial Chemistry Techniques,
pubmed-meshheading:18579375-Crystallography, X-Ray,
pubmed-meshheading:18579375-Drug Design,
pubmed-meshheading:18579375-Enzyme Inhibitors,
pubmed-meshheading:18579375-Ligands,
pubmed-meshheading:18579375-Mass Spectrometry,
pubmed-meshheading:18579375-Models, Chemical,
pubmed-meshheading:18579375-Molecular Structure,
pubmed-meshheading:18579375-Protein-Serine-Threonine Kinases,
pubmed-meshheading:18579375-Purines,
pubmed-meshheading:18579375-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry.
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pubmed:affiliation |
Sunesis Pharmaceuticals, Inc., 395 Oyster Point Boulevard, Suite 400, South San Francisco, CA 94080, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, N.I.H., Extramural
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