环氧酮肽类蛋白酶体抑制剂的研究进展

Research Progress of Epoxyketone Peptidyl Proteasome Inhibitors

随着硼替佐米和卡非佐米被FDA批准用于多发性骨髓瘤患者的治疗,蛋白酶体已成为一种越来越热门的抗肿瘤药物的靶点。环氧酮肽类化合物由于其良好的选择性和较低的不良反应已成为蛋白酶体抑制剂的研究热点。本文主要综述蛋白酶体的结构和功能、环氧酮肽类蛋白酶体抑制剂的作用机制及发展现状。

The approval of proteasome inhibitors-bortezomib and carfilzomib for the treatment of multiple myeloma by FDA validates the potential of proteasome as a promising anti-cancer drug target. Due to the better selectivity and fewer side effects of epoxyketone peptidyl proteasome inhibitors, they have attracted increasing attentions. The structure and function of proteasome and the mechanism of interactions between proteasome and epoxyketone analogues together with the research progress of this series of compounds are going to be reviewed in this manuscript.