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- W3204148409 abstract "An aromatic trifluoromethyl ketone moiety was characterized as a new warhead for covalently reversible kinase inhibitor design to target the non-catalytic cysteine residue. Potent and selective covalently reversible inhibitors of FGFR4 kinase were successfully designed and synthesized by utilizing this new warhead. The binding mode of a representative inhibitor was fully characterized by using multiple technologies including MALDI-TOF mass spectrometry, dialysis assay and X-ray crystallographic studies etc. This functional group was also successfully applied to discovery of a new JAK3 inhibitor, suggesting its potential application in designing other kinase inhibitors." @default.
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- W3204148409 date "2021-11-01" @default.
- W3204148409 modified "2023-10-14" @default.
- W3204148409 title "Characterization of an aromatic trifluoromethyl ketone as a new warhead for covalently reversible kinase inhibitor design" @default.
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- W3204148409 doi "https://doi.org/10.1016/j.bmc.2021.116457" @default.
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