Didehydrofarnesyl diphosphate: an intrinsically fluorescent inhibitor of protein farnesyltransferase |
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Authors: | Liu Xiao-Hui Prestwich Glenn D |
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Affiliation: | Department of Medicinal Chemistry, The University of Utah, 419 Wakara Way, Suite 205, Salt Lake City, UT 84108-1257, USA. |
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Abstract: | Didehydrofarnesyl diphosphate (delta delta FPP), a fluorescent pentaene analogue of farnesyl diphosphate (FPP), was synthesized using stereoselective Wittig reactions. Although delta delta FPP was not an alternative substrate for yeast protein farnesyltransferase (FTase), the fluorescent analogue was a potent competitive inhibitor with a K(i) value of 8.8 microM (K (m) (FPP) = 27 microM). |
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