Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity
Copyright policy )Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity
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.
- University of Pisa Italy
Models, Molecular, Kinetics, Structure-Activity Relationship, Alkyl and Aryl Transferases, Molecular Structure, Polyisoprenyl Phosphates, Diterpenes, Enzyme Inhibitors, Substrate Specificity
Models, Molecular, Kinetics, Structure-Activity Relationship, Alkyl and Aryl Transferases, Molecular Structure, Polyisoprenyl Phosphates, Diterpenes, Enzyme Inhibitors, Substrate Specificity
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