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Reversible Covalent Inhibition of a Protein Target
Author(s) -
Lee ChangUk,
Grossmann Tom N.
Publication year - 2012
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201203341
Subject(s) - covalent bond , electrophile , chemistry , selectivity , combinatorial chemistry , covalent binding , biochemistry , biophysics , organic chemistry , biology , catalysis
Electron‐deficient Michael acceptors can be used in reversible addition/elimination reactions with thiols. These electrophiles were used to convert a known irreversible kinase inhibitor into a covalent and reversible inhibitor. Such an approach might provide high‐affinity binders with increased selectivity without the toxicological risks associated with irreversible protein modifications.