Xie Hao, Liu Junjia, Alem Glison Diego M, Fleming Jason B
Department of Gastrointestinal Oncology, H. Lee Moffitt Cancer Center & Research Institute, Tampa, FL 33612, USA.
Albert Einstein College of Medicine, Bronx, NY 10461, USA.
Explor Target Antitumor Ther. 2021;2(6):511-521. doi: 10.37349/etat.2021.00061. Epub 2021 Dec 31.
Proteolysis targeting chimeras (PROTACs) are a class of small molecules designed to target proteins for degradation. Their novel and unique modes of action provide PROTACs with the potential for their application in the management of both solid and hematologic malignancies. Since its initial discovery, the technology of targeted protein degradation, especially in the form of PROTACs, has had significant advances. A number of PROTACs have entered a late stage of preclinical development. Several of them are either in phase 1/2 clinical trials or approaching approval for initial clinical evaluation. This article discusses the preclinical and clinical findings of PROTACs of clinically relevant protein targets in cancer.
蛋白酶靶向嵌合体（PROTACs）是一类设计用于靶向蛋白质进行降解的小分子。它们新颖独特的作用方式为PROTACs在实体瘤和血液系统恶性肿瘤治疗中的应用提供了潜力。自首次发现以来，靶向蛋白质降解技术，尤其是以PROTACs形式出现的技术，取得了重大进展。许多PROTACs已进入临床前开发的后期阶段。其中一些已进入1/2期临床试验，或即将获批进行初步临床评估。本文讨论了癌症中临床相关蛋白质靶点的PROTACs的临床前和临床研究结果。
