Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China.
Mini Rev Med Chem. 2021;21(16):2290-2299. doi: 10.2174/1389557521666210114163318.
SET protein is a multi-functional oncoprotein that is ubiquitously expressed in most tumor cells. Dysregulation of SET has been associated with many types of cancer. Due to ever-accumulating evidence of its strong correlation with both poor prognosis and drug resistance, the targeting of SET is starting to be explored. SET is currently regarded as a potential target for cancer therapy, and several inhibitors are being developed for clinical trials. In this review, the physiological and pathological functions of SET, as well as its antagonists, will be discussed along with the prospects and challenges involved with translating SET inhibitors into bona fide therapeutic options.
SET 蛋白是一种多功能癌蛋白,在大多数肿瘤细胞中广泛表达。SET 的失调与多种类型的癌症有关。由于越来越多的证据表明其与预后不良和耐药性密切相关,因此开始探索 SET 的靶向治疗。SET 目前被认为是癌症治疗的潜在靶点,正在开发几种抑制剂进行临床试验。在这篇综述中,将讨论 SET 的生理和病理功能及其拮抗剂,以及将 SET 抑制剂转化为真正治疗选择所涉及的前景和挑战。