191801-19-1Relevant academic research and scientific papers
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.
