【摘要】 肿瘤的发生与肿瘤特异癌蛋白的表达密切相关,调控这些蛋白质的降解已成为肿瘤治疗的一种新方法。泛素介导的蛋白质降解通路控制着真核细胞内绝大多数蛋白质的选择性降解。近年来,一种人工合成的蛋白靶向降解嵌合分子(proteolysis targeting chimeric molecule,PROTAC),能通过利用细胞固有的泛素-蛋白酶体系统调控靶向蛋白质降解。本文总结了PROTAC的相关研究进展,虽然对PROTAC技术的研究还有很多尚待解决的问题,但其作为肿瘤治疗的新手段具有很大的潜力。更多还原

【Abstract】 Tumor specific oncoproteins are very important in the development of cancer. One novel approach to eliminate cancer cells is to degrade the oncoproteins. The ubiquitin-dependent proteolysis system (UPS) controls most of the selective protein degradation in all eukaryotic cells. Recently, a new synthetic chimeric molecule (proteolysis targeting chimeric molecule, PROTAC), using the cellular UPS to degrade the oncoproteins, has been developed. Here, we have reviewed the recent advance of PROTAC. Although many problems remain to be solved, PROTAC is a promising strategy to conquer cancer.更多还原