Phosphonoacetamido(oxy) groups have proven to be good mimics of the diphosphate portion in geranylgeranyl protein transferase I (GGTase I) inhibitors. The introduction of small alkyl groups (Me, Et) into the diphosphate mimic moiety caused a further decrease in collateral farnesyl protein transferase (FTase) inhibitory activity, thereby improving GGTase I over FTase selectivity.
Stable analogues of geranylgeranyl diphosphate endowed of improved geranylgeranyl vs. farnesyl protein transferase inhibitory selectivity / F. Minutolo, S. Bertini, L. Betti, R. Danesi, G. G., G. Giannaccini, P. C., G. Placanica, S. Rapposelli, M. Macchia. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 13:24(2003), pp. 4405-4408. [10.1016/j.bmcl.2003.09.035]
Stable analogues of geranylgeranyl diphosphate endowed of improved geranylgeranyl vs. farnesyl protein transferase inhibitory selectivity
R. Danesi;
2003
Abstract
Phosphonoacetamido(oxy) groups have proven to be good mimics of the diphosphate portion in geranylgeranyl protein transferase I (GGTase I) inhibitors. The introduction of small alkyl groups (Me, Et) into the diphosphate mimic moiety caused a further decrease in collateral farnesyl protein transferase (FTase) inhibitory activity, thereby improving GGTase I over FTase selectivity.
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