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 |
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Hauptverfasser: | , , |
Format: | Artikel |
Sprache: | eng |
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Online-Zugang: | Volltext |
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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. |
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ISSN: | 0968-0896 1464-3391 |
DOI: | 10.1016/j.bmc.2016.03.050 |