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

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• 作者：Christian M. Pichler^a ; Joanna Krysiak^b ; Rolf Breinbauer^a ; ^{breinbauer@tugraz.at" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Covalent binding drugs ; Activity based protein profiling ; Target identification ; Biologically active molecules ; Drug targets
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2016
• 出版时间：1 August 2016
• 年：2016
• 卷：24
• 期：15
• 页码：3291-3303
• 全文大小：1598 K

文摘

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.