Discovery of 2-4-dimethoxychalcone as a Hsp90 inhibitor and its effect on iressa-resistant non-small cell lung cancer (NSCLC)

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• 作者：Young Ho Seo
• 关键词：2-4-dimethoxychalcone ; Hsp90 ; Inhibitor ; Iressa ; resistance ; Lung cancer
• 刊名：Archives of Pharmacal Research
• 出版年：2015
• 出版时间：October 2015
• 年：2015
• 卷：38
• 期：10
• 页码：1783-1788
• 全文大小：717 KB
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• 作者单位：Young Ho Seo (1)
  
  1. College of Pharmacy, Keimyung University, Daegu, 704-701, Korea
  
• 刊物主题：Pharmacy; Pharmacology/Toxicology;
• 出版者：Springer Netherlands
• ISSN：1976-3786

文摘

Heat shock protein 90 (Hsp90) is a ATP dependent molecular chaperone and has emerged as an attractive therapeutic target in the war on cancer due to its role in regulating maturation and stabilization of numerous oncogenic proteins. In this study, we discovered that 2-4-dimethoxychalcone (1b) disrupted Hsp90 chaperoning function and inhibited the growth of iressa-resistant non-small cell lung cancer (NSCLC, H1975). The result suggested that 2-4-dimethoxychalcone (1b) could serve as a potential therapeutic lead to circumvent the drug resistance acquired by EGFR mutation and Met amplification. Keywords 2-4-dimethoxychalcone Hsp90 Inhibitor Iressa-resistance Lung cancer