Article
Insights into the negative regulation of EGFR upon the binding of an allosteric inhibitor.
Chemical biology & drug design - 1 Apr 2022
Li Miaomiao, Xu Yan, Guo Jingjing
Abstract excerpt
Epidermal growth factor receptor (EGFR) is an intensively focused drug target for non-small cell lung cancer (NSCLC). JBJ-04-125-02 is an effective ATP-noncompetitive and T790M/L858R-selective inhibitor of EGFR, but the implied negative regulation mechanism is not fully clarified. Here, computational approaches were employed to address this. We find that JBJ-04-125-02 induces contrary effects on the binding of...
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