哺乳动物雷帕霉素靶蛋白(mTOR)是一种丝氨酸/苏氨酸激酶,可集合胞内和胞外信号调节细胞生长、增殖、代谢和存活。在肿瘤的发生发展过程中,mTOR信号多处于异常激活状态,已被确证为肿瘤药物治疗的重要靶标。因雷帕霉素临床应用存在局限性,近期ATP竞争性mTOR抑制剂的研发十分活跃。本文综述了ATP竞争性mTOR抑制剂的研究进展,重点讨论药物的作用特点。 Mammalian target of rapamycin (mTOR) is a serine / threonine kinase that aggregates both intracellular and extracellular signals to regulate cell growth, proliferation, metabolism and survival. In the process of tumorigenesis, mTOR signaling is abnormally activated and has been identified as an important target of oncology drug therapy. Due to the limitations of clinical use of rapamycin, the recent development of ATP-competitive mTOR inhibitors is very active. This article reviews the progress of ATP-competitive mTOR inhibitors, focusing on the role of drugs.