摘要
17-丙烯胺基-17-去甲氧基格尔德霉素(17-AAG)是一种热休克蛋白90(HSP90)抑制剂,能够靶向性抑制肿瘤源性的HSP90,使其效应蛋白即多条细胞信号转导通路的关键调节蛋白降解,从而使细胞生长、分化受抑制,引起细胞凋亡,抑制肿瘤生长。大量试验证明,17-AAG是一种独特的靶向性治疗肿瘤的药物,能有效抑制多条维持肿瘤增殖和生存的细胞信号转导途径。临床Ⅰ-Ⅱ期试验显示该药具有良好的药理作用特征。此外,它还能和放疗、传统化疗药物联合应用协同发挥抗肿瘤作用。
17-allylamino-17-demethoxygeldanamycin （17-AAG） is a heat shock protein 90 （HSP90） inhibitor. It is capable of target-inhibiting tumor-derived HSP90, leading to the depletion of oncogenic client proteins which play key roles in several signal transduction pathways. Then cell growth and differetiation are inhibited. 17-AAG results in cytostasis and apoptosis. A lot of trials have indicated that 17-AAG is a selective target drug for cancer therapy. It can efficiently inhibit multiple signal transduction pathways involved in tumor cell proliferation and survival. Clinical phase Ⅰ and phase Ⅱ trials have shown that 17-AAG has good pharmacokinetic-pharmacodynamic profile. Moreover, it can combine with radiation and the traditional chemotherapeutics and increase the therapeutic efficacy.
出处
《国际肿瘤学杂志》
CAS
2006年第9期646-650,共5页
Journal of International Oncology
基金
国家自然科学基金资助项目(30470500)
关键词
肿瘤
药物疗法
Neoplasms
Drug therapy
