具有改善的香叶基香叶基与法尼基蛋白转移酶抑制选择性的香叶基香叶基二磷酸稳定类似物。
Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity.
作者信息
Minutolo Filippo, Bertini Simone, Betti Laura, Danesi Romano, Gervasi Gianbattista, Giannaccini Gino, Papi Chiara, Placanica Giorgio, Barontini Silvia, Rapposelli Simona, Macchia Marco
机构信息
Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
出版信息
Bioorg Med Chem Lett. 2003 Dec 15;13(24):4405-8. doi: 10.1016/j.bmcl.2003.09.035.
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.
膦酰基乙酰氨基（氧基）基团已被证明是香叶基香叶基蛋白转移酶I（GGTase I）抑制剂中二磷酸部分的良好模拟物。将小烷基（甲基、乙基）引入二磷酸模拟部分会导致法尼基蛋白转移酶（FTase）的旁系抑制活性进一步降低，从而提高GGTase I相对于FTase的选择性。
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