Chen Yi, Ding Jian
Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Science, Chinese Academy of Sciences, Shanghai, 201203, PR China.
Ai Zheng. 2004 Aug;23(8):968-74.
The molecular chaperone heat shock protein 90 (Hsp90) is important in maintaining the conformation, stability, and function of many proteins involved in cell surviving. Hsp90 is of interest as an anticancer drug target because of its importance in maintaining the function of key oncogenic client proteins. Hsp90 inhibitors also have shown promising antitumor activity in vitro and in vivo preclinical model systems. One Hsp90 inhibitor, 17-allylamio-17- desmethoxygeldanamycin (17-AAG), is currently in clinical trial.
分子伴侣热休克蛋白90(Hsp90)对于维持许多参与细胞存活的蛋白质的构象、稳定性及功能至关重要。Hsp90作为抗癌药物靶点备受关注,因为它在维持关键致癌客户蛋白的功能方面具有重要作用。Hsp90抑制剂在体外和体内临床前模型系统中也显示出了有前景的抗肿瘤活性。一种Hsp90抑制剂,17-烯丙胺基-17-去甲氧基格尔德霉素(17-AAG),目前正在进行临床试验。