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SNX-2112, an Hsp90 inhibitor, induces apoptosis and autophagy via degradation of Hsp90 client proteins in human melanoma A-375 cells.
MedLine Citation:
PMID:  22182451     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
SNX-2112 is an Hsp90 inhibitor which is currently undergoing multiple Phase 1 clinical trials; however, its mechanism of action needs to be further elaborated. Here we investigated the effects of SNX-2112 in A-375 cells. SNX-2112 induced the degradation of multiple Hsp90 client proteins, activated both the mitochondrial-mediated and death receptor-mediated apoptotic pathways, downregulated Bcl-2 and Bcl-xL, upregulated Bid, cleaved caspase-9, caspase-7, caspase-3 and PARP, and activated caspase-8. The general caspase inhibitor, z-VAD-fmk, did not completely abolish SNX-2112-induced cell death. SNX-2112 induced autophagy in a time- and dose-dependent manner via Akt/mTOR/p70s6k inhibition. SNX-2112 induces significant apoptosis and autophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent.
Authors:
Kai-Sheng Liu; Hui Liu; Shao-Xiang Wang; Jin-Huan Qi; Qiu-Yun Liu; Zhong Liu; Min Xia; Guo-Wen Xing; Yi-Fei Wang
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-12-16
Journal Detail:
Title:  Cancer letters     Volume:  -     ISSN:  1872-7980     ISO Abbreviation:  -     Publication Date:  2011 Dec 
Date Detail:
Created Date:  2011-12-20     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7600053     Medline TA:  Cancer Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011. Published by Elsevier Ireland Ltd.
Affiliation:
Guangzhoujinan Biomedicine Research and Development Center;Guangdong Provincial Key Laboratory of Bioengineering Medicine;National Engineering Research Center of Genetic Medicine, Jinan University, No.601, West Huangpu Road, Guangzhou 510632, China; Pharmacy College, Jinan University, Guangzhou 510632, China.
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