α-Cyanocinnamide derivatives: a new family of non-peptide, non-sulfhydryl inhibitors of ras farnesylation

E Poradosu, A Gazit, H Reuveni, A Levitzki

Index: Poradosu, Enrique; Gazit, Aviv; Reuveni, Hadas; Levitzki, Alexander Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 8 p. 1727 - 1736

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Citation Number: 8

Abstract

Farnesylation of Ras and other proteins is required for their membrane attachment and normal function. Here we report on the synthesis of α-cyanocinnamide derivatives, a new family of farnesyltransferase inhibitors. These compounds are nonpeptidic and do not contain sulfhydryl groups. The most potent compound is a pure competitive inhibitor with respect to the Ras protein and mixed competitive with respect to farnesyl diphosphate. ...