中文摘要：

微管马达驱动蛋白（kinesin,简称驱动蛋白）是一类沿着微管的特定方向行走的分子马达蛋白家族,在胞内运输和细胞分裂中扮演着重要角色.为了研究驱动蛋白的时空动力学特征,过去近15年的化学生物学研究发掘了一系列特异性的小分子抑制剂,为解析驱动蛋白的系统功能提供了有效的工具.由于部分驱动蛋白在实体瘤中活性异常增高,驱动蛋白小分子抑制剂渐渐发展成为癌症化疗的先导化合物.事实上,基于驱动蛋白Eg5（也叫KIF11）和CENP-E（着丝粒结合蛋白E）的小分子抑制剂已经进入Ⅰ期和Ⅱ期临床实验.本文将简介驱动蛋白的小分子抑制剂研究进展及临床转化研究前景.

英文摘要：

Kinesins are a family of molecular motor proteins that power cargo movements on microtubules using ATP. Kinesins exhibit great diversity in their directional movements and have important roles in cellular transport and mitosis. There has been great excitement and progress in chemical biological studies of kinesins over the past 15 years, which have allowed the development of specific chemical inhibitors to probe the precise functions of individual motor proteins in space and time. Because several kinesins exhibit significantly higher levels and activities in solid tumors compared with normal cells, great efforts are currently centered on translational studies in phase I and phase II clinical trials. In this review, we highlight recent progress in chemical biological studies using Eg5 and CENP-E as major examples and elaborate the translational efforts down the line. We also envisage future developments in this exciting avenue of research.