Target identification of covalently binding drugs by activity-based protein profiling (ABPP)

[Display omitted] The characterization of the target proteins of drug molecules has become an important goal in understanding its mode of action and origin of side effects due to off-target binding. This is especially important for covalently binding drugs usually containing electrophilic moieties,...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2016-08, Vol.24 (15), p.3291-3303
Hauptverfasser: Pichler, Christian M., Krysiak, Joanna, Breinbauer, Rolf
Format: Artikel
Sprache:eng
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Zusammenfassung:[Display omitted] The characterization of the target proteins of drug molecules has become an important goal in understanding its mode of action and origin of side effects due to off-target binding. This is especially important for covalently binding drugs usually containing electrophilic moieties, which potentially can react with nucleophilic residues found in many proteins. This review gives a comprehensive overview of the use of activity-based protein profiling (ABPP) as an efficient tool for the target identification of covalently binding drugs.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2016.03.050