[HTML][HTML] Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation

A Wang, XE Yan, H Wu, W Wang, C Hu, C Chen… - Oncotarget, 2016 - ncbi.nlm.nih.gov
Ibrutinib, a clinically approved irreversible BTK kinase inhibitor for Mantle Cell Lymphoma
(MCL) and Chronic Lymphocytic Leukemia (CLL) etc, has been reported to be potent
against EGFR mutant kinase and currently being evaluated in clinic for Non Small Cell Lung
Cancer (NSCLC). Through EGFR wt/mutant engineered isogenic BaF3 cell lines we
confirmed the irreversible binding mode of Ibrutinib with EGFR wt/mutant kinase via Cys797.
However, comparing to typical irreversible EGFR inhibitor, such as WZ4002, the washing …

[引用][C] Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation. Oncotarget 7: 69760–69769

A Wang, XE Yan, H Wu - 2016
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