Chitkara College of Pharmacy, Chitkara University, Rajpura, Patiala, Punjab, India.
Mini Rev Med Chem. 2021;21(16):2347-2360. doi: 10.2174/1389557521666210226150740.
Cancer treatment has become a major challenge amidst the resistance and relapse caused by the various treatments available. The PROteolysis TAargeting Chimera (PROTAC) technology involves the degradation of target protein against the inhibition by small drug molecules. The PROTACs with high potency and activity have been frequently reported; however, no PROTAC acting against cancer has reached the clinical trials. The concept of PROTACs involves the reduction in the disease-causing protein by its degradation through the ubiquitin-proteasomal enzyme system. This concept has attracted a lot of attention from both industry and academia due to its potential in drug discovery (in the form of PROTACs), which can conquer the resistance associated with current treatments of cancer. Thus, it is the need of the hour to identify and synthesize more PROTACs for a viable treatment of cancer. This article reviews the design, activity and effects produced in cancer by some recently developed PROTACs.
癌症治疗已成为一个主要的挑战，因为现有的各种治疗方法都存在耐药性和复发的问题。蛋白水解靶向嵌合体（PROTAC）技术涉及到用小分子药物抑制目标蛋白的降解。已经有很多报道称具有高效力和活性的 PROTAC，但没有针对癌症的 PROTAC 达到临床试验阶段。PROTAC 的概念涉及通过泛素-蛋白酶体酶系统降解致病蛋白来减少疾病。由于其在药物发现（PROTAC 形式）方面的潜力，这一概念引起了工业界和学术界的广泛关注，因为它可以克服当前癌症治疗相关的耐药性。因此，现在需要识别和合成更多的 PROTAC 来治疗癌症。本文综述了一些最近开发的 PROTAC 在癌症中的设计、活性和作用。
