正碳离子样的过渡态类似物研究进展

The Development of the Carbenium Transition State Analogs

综述了应用酶催化过渡态理论设计的几类正碳离子样的过渡态类似物作为酶的抑制剂的研究进展。其中包括类异戊二烯的正离子过渡态类似物,唾液酸转移酶的过渡态类似物,3-脱氧-D-甘露糖-2-辛酮糖酸酯-8-磷酸酯(KDO8P)合成酶的过渡态类似物,尿苷二磷酸酯葡糖醛酸基转移酶(UGT)的过渡态类似物。

An important feature in the enzyme catalyzed reaction is that an enzyme recognizes and binds more tightly to the transition state than to the ground state of the substrate product interconversion. The transition state analog must be a potent inhibitor of the enzyme. The recent development of the carbenium transition state analogs as the enzymatic inhibitors which are designed by the transition state theory of enzyme catalyzed reactions is reviewed. Four types of enzymatic inhibitors including the transition state analogs of isoprenoid pyrophosphate, sialyltransferase, KDO8P and UGT are introduced.