Linked Life Data

16107140

Source:http://linkedlifedata.com/resource/pubmed/id/16107140

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pubmed-article:16107140pubmed:abstractTextTipifarnib (R115777), an inhibitor of human protein farnesyltransferase (PFT), is shown to be a highly potent inhibitor of Trypanosoma cruzi growth (ED(50) = 4 nM). Surprisingly, this is due to the inhibition of cytochrome P450 sterol 14-demethylase (CYP51, EC 1.14.13.70). Homology models of the T. cruzi CYP51 were used for the prediction of the binding modes of the substrate lanosterol and of Tipifarnib, providing a basis for the design of derivatives with selectivity for TcCYP51 over human PFT.lld:pubmed
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pubmed-article:16107140pubmed:articleTitleThe protein farnesyltransferase inhibitor Tipifarnib as a new lead for the development of drugs against Chagas disease.lld:pubmed
pubmed-article:16107140pubmed:affiliationDepartment of Biochemistry, University of Washington, Seattle, Washington 98195, USA.lld:pubmed
pubmed-article:16107140pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:16107140pubmed:publicationTypeResearch Support, U.S. Gov't, P.H.S.lld:pubmed
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