【摘要】 泛素-蛋白酶体系统(UPS)的失控与肿瘤、神经退行性疾病、病毒感染等疾病密切相关,以该系统为导向的药物研发已逐渐引发关注,其中蛋白酶体抑制剂硼替佐米(万珂)作为抗肿瘤药物已成功上市。泛素特异性蛋白酶7(USP7)是UPS中的一种关键性酶,作为去泛素化酶参与细胞内肿瘤抑制、DNA修复及免疫应答等过程中诸多重要蛋白的活性调控。本文介绍泛素特异性蛋白酶7及其抑制剂,强调泛素特异性蛋白酶7抑制剂在抗肿瘤治疗中的潜在应用价值。更多还原

【Abstract】 Deregulation of the ubiquitn-proteasome system( UPS) is linked to pathogenesis of various human diseases including cancer,neurodegenerative disorders and viral diseases. UPS-based drug discovery has gradually attracted attention as evidenced by the approval of proteasome inhibitor bortezomib( Velcade) as an anticancer drug. Ubiquitin-specific protease 7( USP7),a key deubiquitinase in UPS,is involved in activity regulation of numerous proteins that play crucial roles in tumor suppression,DNA repair,immune responses, etc. Herein USP7 and its inhibitors to raise concern about the potential application of USP7 inhibitors as anticancer therapy w ere introduced.更多还原