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  • Year in Review
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Targeted covalent inhibitors in 2023

Tying the knot with lysine

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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Correspondence to Ana Koperniku.

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Koperniku, A., Meanwell, N.A. Tying the knot with lysine. Nat Rev Chem 8, 235–237 (2024).

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