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Targeted covalent inhibitors in 2023

Tying the knot with lysine

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Targeted covalent inhibitors (TCIs) can react irreversibly with lysine in kinases and other proteins. Small molecule TCIs can have both broad or specific lysine targeting whereas peptide- and protein-based TCIs were shown to provide high target specificity for lysines in shallow protein surfaces.

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Fig. 1: Targeted covalent inhibitors in reaction lysine.

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Authors and Affiliations

  1. The Center for the Study of Language and Information, Stanford University, Stanford, CA, USA

    Ana Koperniku

  2. The Baruch S. Blumberg Insitute, Doylestown, PA, USA

    Nicholas A. Meanwell

  3. The School of Pharmacy, The University of Michigan, Ann Arbor, MI, USA

    Nicholas A. Meanwell

Authors
  1. Ana Koperniku
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  2. Nicholas A. Meanwell
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Correspondence to Ana Koperniku.

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The authors declare no competing interests.

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Koperniku, A., Meanwell, N.A. Tying the knot with lysine. Nat Rev Chem 8, 235–237 (2024). https://doi.org/10.1038/s41570-024-00592-4

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