Article
Inhibition of farnesyltransferase with A-176120, a novel and potent farnesyl pyrophosphate analogue.
European journal of cancer (Oxford, England : 1990) - 1 Jun 2000
Tahir S K, Gu W Z, Zhang H C, Leal J, Lee J Y, Kovar P, Saeed B, Cherian S P, Devine E, Cohen J, Warner R, Wang Y C, Stout D, Arendsen D L, Rosenberg S, Ng S C
Abstract excerpt
Farnesylation of Ras is required for its transforming activity in human cancer and the reaction is catalysed by the enzyme farnesyltransferase. Recently, we discovered a novel chemical series of potent farnesyl pyrophosphate (FPP) analogues which selectively inhibited farnesyltransferase. Our most potent compound to date in this series, A-176120, selectively inhibited farnesyltransferase activity (IC(50)...
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