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KINASE INHIBITORS

Tuned out

Nature Chemical Biology volume 18, pages 917–918 (2022)Cite this article

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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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Authors and Affiliations

  1. Department of Chemistry & Biochemistry, and the Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, San Diego, CA, USA

    Fleur M. Ferguson

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  1. Fleur M. Ferguson
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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 18, 917–918 (2022). https://doi.org/10.1038/s41589-022-01037-z

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