191801-19-1Relevant articles and documents
Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity
Minutolo, Filippo,Bertini, Simone,Betti, Laura,Danesi, Romano,Gervasi, Gianbattista,Giannaccini, Gino,Papi, Chiara,Placanica, Giorgio,Barontini, Silvia,Rapposelli, Simona,Macchia, Marco
, p. 4405 - 4408 (2003)
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.