摘要
17-丙烯胺基-17-去甲氧基格尔德霉素(17-AAG)及衍生物17-AAGH2、17-DMAG是热休克蛋白90竞争性抑制剂,能够降解多条信号传导通路关键蛋白,抑制肿瘤细胞生长,促使凋亡。临床Ⅰ-Ⅱ期研究证明,17-AAG及衍生物能够抑制T790M表达类型肺癌细胞,抑制肺癌细胞表皮生长因子受体,协同化疗药物细胞毒性、放射增敏作用。
17-allylamino- 17-demethoxygeldanamycin(17-AAG) as well as its derivatives 17-AAGH2 and 17-DMAG are heat shock protein90 inhibitor. It can lead to the depletion of oncogenie client proteins which play key roles in several signal transductions pathways. Cell growth is inhibited and apoptosis is predicated. Clinical phase Ⅰ and phase Ⅱ trials indicate 17-AAG and its derivatives can efficiently inhibit lung cancer cells expressing T790M and epidermal growth 'factor, coordinate with chemotherapeutics cytotoxicity and increase radiosensitizing effect.
出处
《国际肿瘤学杂志》
CAS
2009年第8期601-604,共4页
Journal of International Oncology
基金
基金项目:国家自然科学基金资助项目(30470500)