Article
Gefitinib analogue V1801 induces apoptosis of T790M EGFR-harboring lung cancer cells by up-regulation of the BH-3 only protein Noxa.
PloS one - 1 Jan 2012
Zhang Bo, Jiao Jiao, Liu Ying, Guo Liang-Xia, Zhou Bo, Li Gang-Qin, Yao Zhu-Jun, Zhou Guang-Biao
Abstract excerpt
Treatment of non-small cell lung cancer (NSCLC) with drugs targeting the epidermal growth factor receptor (EGFR), e.g., gefitinib and erlotinib, will eventually fail because of the development of secondary mutations such as T790M in EGFR. Strategies to overcome this resistance are therefore an urgent need. In this study, we synthesized a dozen of novel gefitinib analogues and evaluated their effects on...
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