T790米
奥西默替尼
第三代
癌症研究
突变
化学
抗药性
药理学
表皮生长因子受体
癌症
医学
埃罗替尼
生物
遗传学
吉非替尼
内科学
基因
生物化学
电信
计算机科学
作者
Harun Patel,Rahul Pawara,Azim Ansari,Sanjay J. Surana
标识
DOI:10.1016/j.ejmech.2017.05.027
摘要
EGFR T790M mutation leads to resistance to most of clinically available EGFR TKIs. Third-generation EGFR TKIs against the T790M mutation have been in active clinical development, which includes osimertinib, rociletinib, HM61713, ASP8273, EGF816, and PF-06747775. On the other hand recently EGFR C797S mutation was reported to be a leading mechanism of resistance to the third-generation inhibitors. The C797S mutation appears to be an ideal target for overcoming the acquired resistance to the third generation inhibitors. This review summarizes the third generation inhibitors, synthesis, their mechanism of resistance and latest development on the discovery of a fourth-generation EGFR TKIs and U to Y allosteric strategies to combat the C797S EGFR resistance problem.
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