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KINASE INHIBITORS

Tuned out

Controlling kinase inhibitors’ residence time via reversible covalent binding is of high interest in drug discovery. Tuning reversible covalent binding kinetics using a pan-kinase inhibitor that reacts with the catalytic lysine enabled exquisite temporal selectivity in vitro and in vivo.

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Fig. 1: Reversible covalent targeting of catalytic lysines enables residence-time-based selectivity across the kinome.

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Correspondence to Fleur M. Ferguson.

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Competing interests

F.F. is a scientific co-founder and equity holder in Proximity Therapeutics, and a scientific advisory board member and equity holder in Triana Biomedicines. F.F. is or was recently a consultant or received speaking honoraria from RA Capital, Tocris BioTechne and Plexium Inc. The Ferguson lab receives or has received research funding from Ono Pharmaceutical Co. Ltd.

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Ferguson, F.M. Tuned out. Nat Chem Biol (2022). https://doi.org/10.1038/s41589-022-01037-z

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  • DOI: https://doi.org/10.1038/s41589-022-01037-z

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