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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
20
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pubmed:dateCreated |
2004-9-16
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pubmed:abstractText |
The first nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S (CatS) are described. Electronic database searching using the program DOCK generated a screening set of potential CatS inhibitors from which two lead structures were identified as promising starting points for a drug discovery effort. Lead optimization afforded potent (IC(50) < 50 nM) and selective inhibitors of CatS demonstrating cellular activity and reversibility of enzyme inhibition.
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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 |
Sep
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
23
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pubmed:volume |
47
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4799-801
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:15369380-B-Lymphocytes,
pubmed-meshheading:15369380-Cathepsins,
pubmed-meshheading:15369380-Cells, Cultured,
pubmed-meshheading:15369380-Cysteine Proteinase Inhibitors,
pubmed-meshheading:15369380-Drug Evaluation, Preclinical,
pubmed-meshheading:15369380-Histocompatibility Antigens Class II,
pubmed-meshheading:15369380-Humans,
pubmed-meshheading:15369380-Immunoglobulin Constant Regions,
pubmed-meshheading:15369380-Inhibitory Concentration 50,
pubmed-meshheading:15369380-Peptides,
pubmed-meshheading:15369380-Protein Conformation,
pubmed-meshheading:15369380-Structure-Activity Relationship
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pubmed:year |
2004
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pubmed:articleTitle |
Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S.
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pubmed:affiliation |
Johnson & Johnson Pharmaceutical Research and Development L.L.C., 3210 Merryfield Row, San Diego, California 92121, USA.
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pubmed:publicationType |
Journal Article
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