title: Target identification of covalently binding drugs by activity-based protein profiling (ABPP).
abstract: 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.
authors.affiliation: Institute of Organic Chemistry, Graz University of Technology, Stremayrgasse 9, 8010 Graz, Austria.
authors.forename: Christian M
authors.initials: CM
authors.lastname: Pichler
authors.affiliation: Department of Chemistry, Technische Universität München, Lichtenbergstraße 4, 85748 Garching, Germany.
authors.forename: Joanna
authors.initials: J
authors.lastname: Krysiak
authors.affiliation: Institute of Organic Chemistry, Graz University of Technology, Stremayrgasse 9, 8010 Graz, Austria. Electronic address: breinbauer@tugraz.at.
authors.forename: Rolf
authors.initials: R
authors.lastname: Breinbauer
mesh_terms: D000818:Animals; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D058990:Molecular Targeted Therapy / Q000379:methods*; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000378:metabolism*; D011485:Protein Binding; D011506:Proteins / Q000737:chemistry* / Q000378:metabolism*
chemical_list: D004364:Pharmaceutical Preparations; D011506:Proteins
keywords: Activity based protein profiling; Biologically active molecules; Covalent binding drugs; Drug targets; Target identification