Journal
TRENDS IN PHARMACOLOGICAL SCIENCES
Volume 44, Issue 7, Pages 474-488Publisher
CELL PRESS
DOI: 10.1016/j.tips.2023.04.007
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Covalent modification of target proteins by specific residue labeling is a promising approach for obtaining small-molecule modulators of PPIs with appropriate selectivity and duration of action.
The development of small-molecule inhibitors or stabilizers of selected protein- protein interactions (PPIs) of interest holds considerable promise for the devel-opment of research tools as well as candidate therapeutics. In this context, the covalent modification of selected residues within the target protein has emerged as a promising mechanism of action to obtain small-molecule modulators of PPIs with appropriate selectivity and duration of action. Different covalent labeling strategies are now available that can potentially allow for a rational, ground-up discovery and optimization of ligands as PPI inhibitors or stabilizers. This review article provides a synopsis of recent developments and applications of such tac-tics, with a particular focus on site-directed fragment tethering and proximity -enabled approaches.
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