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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
1999-2-23
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pubmed:abstractText |
Farnesyl-protein transferase (FPTase) catalyses the specific transfer of farnesyl to Ras-peptides that is essential for oncogenic activity in oncogene-mediated tumors. Specific inhibition of FPTase activity has been shown to reduce tumor development in nude mice challenged with oncogenic forms of ras, thereby establishing FPTase as a viable therapeutic target. Our continued efforts to discover inhibitors of FPTase has led to the discovery of a triterpenoidal inhibitor, clavaric acid (1). This compound inhibits rHFPTase with an IC50 value of 1.3 microM. Structure elucidation, structure modifications, and biological activity of clavaric acid are herein described.
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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 |
Dec
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pubmed:issn |
0163-3864
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
61
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1568-70
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:9868169-Alkyl and Aryl Transferases,
pubmed-meshheading:9868169-Animals,
pubmed-meshheading:9868169-Basidiomycota,
pubmed-meshheading:9868169-Enzyme Inhibitors,
pubmed-meshheading:9868169-Fermentation,
pubmed-meshheading:9868169-Hydrolysis,
pubmed-meshheading:9868169-Lanosterol,
pubmed-meshheading:9868169-Methylation,
pubmed-meshheading:9868169-Mice,
pubmed-meshheading:9868169-Spectrophotometry, Infrared
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pubmed:year |
1998
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pubmed:articleTitle |
Clavaric acid: a triterpenoid inhibitor of farnesyl-protein transferase from Clavariadelphus truncatus.
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pubmed:affiliation |
Natural Products Drug Discovery, Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA.
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pubmed:publicationType |
Journal Article
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