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Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation.
Wang A, Yan XE, Wu H, Wang W, Hu C, Chen C, Zhao Z, Zhao P, Li X, Wang L, Wang B, Ye Z, Wang J, Wang C, Zhang W, Gray NS, Weisberg EL, Chen L, Liu J, Yun CH, Liu Q. Wang A, et al. Among authors: zhao z, zhao p. Oncotarget. 2016 Oct 25;7(43):69760-69769. doi: 10.18632/oncotarget.11951. Oncotarget. 2016. PMID: 27626175 Free PMC article.
Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells.
Wu H, Wang A, Zhang W, Wang B, Chen C, Wang W, Hu C, Ye Z, Zhao Z, Wang L, Li X, Yu K, Liu J, Wu J, Yan XE, Zhao P, Wang J, Wang C, Weisberg EL, Gray NS, Yun CH, Liu J, Chen L, Liu Q. Wu H, et al. Among authors: zhao z, zhao p. Oncotarget. 2015 Oct 13;6(31):31313-22. doi: 10.18632/oncotarget.5182. Oncotarget. 2015. PMID: 26375053 Free PMC article.
Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.
Wang A, Li X, Wu H, Zou F, Yan XE, Chen C, Hu C, Yu K, Wang W, Zhao P, Wu J, Qi Z, Wang W, Wang B, Wang L, Ren T, Zhang S, Yun CH, Liu J, Liu Q. Wang A, et al. Among authors: zhao p. J Med Chem. 2017 Apr 13;60(7):2944-2962. doi: 10.1021/acs.jmedchem.6b01907. Epub 2017 Mar 22. J Med Chem. 2017. PMID: 28282122
Structural pharmacological studies on EGFR T790M/C797S.
Kong LL, Ma R, Yao MY, Yan XE, Zhu SJ, Zhao P, Yun CH. Kong LL, et al. Among authors: zhao p. Biochem Biophys Res Commun. 2017 Jun 24;488(2):266-272. doi: 10.1016/j.bbrc.2017.04.138. Epub 2017 Apr 26. Biochem Biophys Res Commun. 2017. PMID: 28456628
9,547 results