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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: ye z. 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: ye z. Oncotarget. 2015 Oct 13;6(31):31313-22. doi: 10.18632/oncotarget.5182. Oncotarget. 2015. PMID: 26375053 Free PMC article.
Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor.
Liang X, Lv F, Wang B, Yu K, Wu H, Qi Z, Jiang Z, Chen C, Wang A, Miao W, Wang W, Hu Z, Liu J, Liu X, Zhao Z, Wang L, Zhang S, Ye Z, Wang C, Ren T, Wang Y, Liu Q, Liu J. Liang X, et al. Among authors: ye z. J Med Chem. 2017 Mar 9;60(5):1793-1816. doi: 10.1021/acs.jmedchem.6b01413. Epub 2017 Feb 14. J Med Chem. 2017. PMID: 28140585
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