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- W3114202005 abstract "Ibrutinib is a BTK-targeted irreversible inhibitor. In this study, we demonstrate that ibrutinib potently inhibits SRC activity in a non-covalent manner via mass spectrometry and crystallography. The S345C mutation renders SRC to bind covalently with ibrutinib, and restores the potency of ibrutinib against the gatekeeper mutant. The co-crystal structure of ibrutinib/SRC shows Ser345 of SRC did not form covalent bond with ibrutinib, leading to a decrease of potency and loss of the ability to overcome the gatekeeper mutation of SRC. The X-ray crystallographic studies also provide structural insight into why ibrutinib behaves differently against gatekeeper mutants of different kinases." @default.
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- W3114202005 date "2021-02-01" @default.
- W3114202005 modified "2023-09-28" @default.
- W3114202005 title "Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases" @default.
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- W3114202005 doi "https://doi.org/10.1016/j.bmcl.2020.127757" @default.
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