纺锤体驱动蛋白抑制剂研究进展

摘要

Kinesin spindle protein (KSP) is an essential kinesin to mitotic spindle formation. KSP inhibitors could arrest cell cycle progression and the proliferation of tumor cells and to be novel antimitotic agents. Today, a lot of KSP inhibitors have been developed, and some even entered the clinical stage. This review briefly describes the biology of KSP and its inhibitors, and divides different KSP inhibitors into four types, including pyrimidone, pyrazoline/ pyrroline, polynucleation, and so on, while covering their research advances.%纺锤体驱动蛋白(kinesin spindle protein,KSP)是一种对有丝分裂纺锤体的形成起关键作用的驱动蛋白,其抑制剂能阻碍细胞周期正常分裂、控制肿瘤细胞的增殖,是一类新的抗有丝分裂药物.近几年来很多靶向KSP的抑制剂被相继开发,有的已经进入临床研究阶段.文中概述了KSP及其抑制剂的生物学基础,并将各种结构类型的KSP抑制剂分为嘧啶酮、二氢吡唑/吡咯、多环等4大类,综述了其研究概况.