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
MINUTOLO, FILIPPO;BERTINI, SIMONE;BETTI, LAURA;DANESI, ROMANO;GIANNACCINI, GINO;PLACANICA, GIORGIO;RAPPOSELLI, SIMONA;MACCHIA, MARCO
2003-01-01
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.File in questo prodotto:
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