TY - JOUR
T1 - α-Cyanocinnamide derivatives
T2 - A new family of non-peptide, non-sulfhydryl inhibitors of ras farnesylation
AU - Poradosu, Enrique
AU - Gazit, Aviv
AU - Reuveni, Hadas
AU - Levitzki, Alexander
PY - 1999/8
Y1 - 1999/8
N2 - 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. Selectivity studies against geranylgeranyltransferase and biological activities of selected compounds are described. Copyright (C) 1999.
AB - 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. Selectivity studies against geranylgeranyltransferase and biological activities of selected compounds are described. Copyright (C) 1999.
UR - https://www.scopus.com/pages/publications/0032769472
U2 - 10.1016/S0968-0896(99)00118-2
DO - 10.1016/S0968-0896(99)00118-2
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C2 - 10482464
AN - SCOPUS:0032769472
SN - 0968-0896
VL - 7
SP - 1727
EP - 1736
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 8
ER -
