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

作者：Seo Young Ho^*

来源：Archives of Pharmacal Research, 2015, 38(10): 1783-1788.

DOI：10.1007/s12272-015-0595-6

• 2 ',4 '-dimethoxychalcone
• Hsp90
• Inhibitor
• Iressa-resistance
• Lung cancer

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.

• 出版日期2015-10