摘要
热休克蛋白90(heatshockprotein90,Hsp90)作为分子伴侣参与调控、维持细胞内多种蛋白的构象和功能,以帮助细胞在应激环境刺激下正常生长。近年来研究表明很多癌基因蛋白均为Hsp90的作用靶点,因此抑制Hsp90的功能将促进这些癌基因蛋白的降解,有助于癌症治疗。体内外实验也证实了Hsp90抑制剂的抗肿瘤活性,其中17-烯丙胺-17-脱甲氧格尔德霉素(17-allylamio-17-desmethoxygeldanamycin,17-AAG)正在进行临床试验。
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.
出处
《癌症》
SCIE
CAS
CSCD
北大核心
2004年第8期968-974,共7页
Chinese Journal of Cancer