Advancing Covalent Ligand and Drug Discovery beyond Cysteine
Covalent Modifiers
JUNE 5, 2025
Gibae Kim, R. Justin Grams, and Ku-Lung Hsu Chemical Reviews 2025 DOI: 10.1021/acs.chemrev.5c00001 Targeting intractable proteins remains a key challenge in drug discovery, as these proteins often lack well-defined binding pockets or possess shallow surfaces not readily addressed by traditional drug design. Covalent chemistry has emerged as a powerful solution for accessing protein sites in difficult to ligand regions.
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