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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
2010-6-3
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pubmed:abstractText |
A series of small molecules bearing an alpha-ketoamide warhead were synthesized and evaluated for their ability to inhibit cathepsin S, a key proteolytic enzyme upregulated in many cancers during tumor progression and metastasis. Most of the synthetic compounds were noncytotoxic, but several robustly inhibited cathepsin S (IC(50) < 10 nM) and potently suppressed cell migration, invasion, and capillary tube formation. These results highlight the potential of alpha-ketoamide therapy for preventing or delaying cancer spread.
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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 |
Jun
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:ChangJang-YangJY,
pubmed-author:ChangMargaret Dah-TsyrMD,
pubmed-author:ChangWun-Shaing WayneWS,
pubmed-author:ChangYi-HsunYH,
pubmed-author:ChenJo-ChunJC,
pubmed-author:ChengChao-ShengCS,
pubmed-author:HsiehHsing-PangHP,
pubmed-author:KuoChing-ChuanCC,
pubmed-author:LinChun-ChengCC,
pubmed-author:LiuKo-JiunnKJ,
pubmed-author:LyuPing-ChiangPC,
pubmed-author:UangBiing-JiunBJ,
pubmed-author:WangHsin-ChiehHC
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pubmed:issnType |
Electronic
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pubmed:day |
10
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pubmed:volume |
53
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4545-9
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pubmed:meshHeading |
pubmed-meshheading:20481438-Amides,
pubmed-meshheading:20481438-Cathepsins,
pubmed-meshheading:20481438-Cell Line, Tumor,
pubmed-meshheading:20481438-Drug Design,
pubmed-meshheading:20481438-Humans,
pubmed-meshheading:20481438-Models, Molecular,
pubmed-meshheading:20481438-Neoplasm Invasiveness,
pubmed-meshheading:20481438-Neoplasms,
pubmed-meshheading:20481438-Neovascularization, Pathologic,
pubmed-meshheading:20481438-Protease Inhibitors,
pubmed-meshheading:20481438-Protein Conformation
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pubmed:year |
2010
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pubmed:articleTitle |
Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis.
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pubmed:affiliation |
Department of Chemistry, National Tsing Hua University, 101, Section 2, Kuang-Fu Road, Hsinchu 30013, Taiwan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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