蛋白酶体抑制剂的研究进展  

The Research Progress of Proteasome Inhibitors

作　　者：贾光伟[1] 袁红[1] 李爱波[1] 杜蕾[1] 吴峰[1] 李玉艳[1] 

机构地区：[1]中国药科大学药学院药物化学教研室,江苏南京210009

出　　处：《精细化工中间体》2012年第6期6-11,共6页Fine Chemical Intermediates

基　　金：国家自然科学基金青年项目(81102317);2011年度中国药科大学"先声药业研究生创新基金"项目(YCX11S001XS)

摘　　要：随着近期美国食品和药物管理局(FDA)批准将Carfilzomib用于难治性多发性骨髓瘤患者的治疗,20 S蛋白酶体已经成为一种越来越引人关注的肿瘤治疗靶标。目前,已经开发出了一系列低纳摩尔浓度的合成和天然20 S蛋白酶体抑制剂,作为抗癌和抗炎的药物进入各期临床实验。此外,蛋白酶抑制剂继续作为有价值的研究工具,通过阐明蛋白质在泛素-蛋白酶体降解途径这一重要的生物学过程,在细胞生物学中发挥作用。With the approval of carfilzomib for the treatment of refractory multiple myeloma patients by FDA,the proteasome has been become one of the most attractive targets for treatment of cancer.So far,a vast array of synthetic and natural compounds have been developed with low nanomolar activity as the 20S proteasome inhibitors and entered pre-clinic or clinical trials as anti-cancer and anti-inflammatory agents.In addition,the protease inhibitors are used as the research tool to clarify the process of protein degradation in the ubiquitin proteasome pathway.This review will highlight the latest progress on the research of proteasome inhibitor.

关 键 词：蛋白酶体 蛋白酶体抑制剂 硼替佐米 Carfilzomib 

分 类 号：R977.6[医药卫生—药品]