Skip to main content
editorial
. 2015 Dec 18;7(1):2–5. doi: 10.1021/acsmedchemlett.5b00475

Figure 1.

Figure 1

(A) Chemical structures of representative examples of the three generations of EGFR inhibitors currently used in the treatment of NSCLC. The reactive acrylamides are highlighted in green. (B) Illustration of the steric repulsion of the first-generation inhibitor gefitinib upon T790M gatekeeper mutation. The gefitinib binding pose observed with EGFR wild type (white, PDB code: 2ITY) would lead to a steric clash with the methionine side chain (blue, PDB code: 3UG1), resulting in an unfavored binding pose (pink, PDB code: 3UG2).