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Furan Warheads For Covalent Trapping Of Weak Protein–protein Interactions: Cross-linking Of Thymosin β4 To Actin

Laia Miret-Casals, Willem Vannecke, Kurt Hoogewijs, Gianluca Arauz-Garofalo, Marina Gay, Mireia Díaz-Lobo, Marta Vilaseca, Christophe Ampe, Marleen Van Troys, Annemieke Madder

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Furan is used as a caged warhead to covalently target weak protein–protein interactions. Furan-thymosin β4 cross-links selectively and irreversibly with actin targeting lysine. Furan technology could be further exploited for covalent drug design.