近年来蛋白靶向降解（PROTAC）技术作为一种新的治疗手段在抗肿瘤药物领域中得到了广泛的研究。PROTAC是一种双功能的小分子化合物，可以将靶蛋白与E3泛素连接酶连接形成三元复合物，通过泛素-蛋白酶体系降解靶蛋白。雌激素（ER）、雄激素（AR）、间变性淋巴瘤激酶（ALK）、布鲁顿酪氨酸激酶（BTK）、溴结构域蛋白4（BRD4）和细胞周期蛋白依赖激酶8（CDK8）等多种蛋白已经被选为靶蛋白进行了研究。对PROTAC的小分子抗肿瘤药物的研究进展进行综述。

In recent years, proteolysis targeting chimera(PROTAC), as a new therapeutic method, has been widely studied in the field of anti-cancer drugs. PROTAC is a bifunctional small molecule compound, which can connect target protein with E3 ubiquitin ligase to form ternary complex, and degrade target protein through ubiquitin-protease system. Estrogen (ER), androgen (AR), anaplastic lymphoma kinase (ALK), bromine domain protein 4 (BRD4), and cyclin dependent kinase 8 (CDK8) have been selected as target proteins for a large number of studies. Research progress on small molecule anti-cancer drugs of PROTAC is reviewed in this paper.

中央高校基本科研业务费专项资金资助项目（3332018117）；中国医学科学院医学与健康科技创新工程项目（2016-I2M-3-022和2017-I2M-3-019）