Nicos A. PETASIS,Florence M. HOFMAN,Stan G. LOUIE,Thomas C. CHEN,Axel H. SCHONTHAL
申请号：
US14109731
公开号：
US20140295549A1
申请日:
2013.12.17
申请国别(地区):
US
年份:
2014
代理人:
摘要：
The present invention provides a method for inducing apoptosis in selected cells by aggravating ER-stress. The aggravation of ER-stress is achieved in a specific manner by inhibiting SERCA (sarcoplasmic/endoplasmic reticulum calcium ATPase), leading to elevated level of cytoplasmic calcium concentration, yet without inhibiting the activity of COX-2 (cyclooxygenase-2) or triggering the release of histamine. Induction of apoptosis may be enhanced by first inducing or further aggravating ER-stress through inhibition of proteasome or proteases. Also provided are compounds and compositions useful as ER-stress aggravating agents, methods for screening, selecting, identifying and designing the same and methods for treating diseased conditions by inducing apoptosis through specific and selective aggravation of ER-stress.
