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      Activity-based protein profiling: A graphical review

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          Abstract

          Activity-based protein profiling (ABPP) is a chemoproteomic technology that employs small chemical probes to directly interrogate protein function within complex proteomes. Since its initial application almost 25 years ago, ABPP has proven to be a powerful and versatile tool for addressing numerous challenges in drug discovery, including the development of highly selective small-molecule inhibitors, the discovery of new therapeutic targets, and the illumination of target proteins in tissues and organisms. This graphical review provides an overview of the rapid evolution of ABPP strategies, highlighting the versatility of the approach with selected examples of its successful application.

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          Click Chemistry: Diverse Chemical Function from a Few Good Reactions

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            Bioorthogonal chemistry: fishing for selectivity in a sea of functionality.

            The study of biomolecules in their native environments is a challenging task because of the vast complexity of cellular systems. Technologies developed in the last few years for the selective modification of biological species in living systems have yielded new insights into cellular processes. Key to these new techniques are bioorthogonal chemical reactions, whose components must react rapidly and selectively with each other under physiological conditions in the presence of the plethora of functionality necessary to sustain life. Herein we describe the bioorthogonal chemical reactions developed to date and how they can be used to study biomolecules.
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              Activity-based protein profiling: from enzyme chemistry to proteomic chemistry.

              Genome sequencing projects have provided researchers with a complete inventory of the predicted proteins produced by eukaryotic and prokaryotic organisms. Assignment of functions to these proteins represents one of the principal challenges for the field of proteomics. Activity-based protein profiling (ABPP) has emerged as a powerful chemical proteomic strategy to characterize enzyme function directly in native biological systems on a global scale. Here, we review the basic technology of ABPP, the enzyme classes addressable by this method, and the biological discoveries attributable to its application.
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                Author and article information

                Contributors
                Journal
                Curr Res Pharmacol Drug Discov
                Curr Res Pharmacol Drug Discov
                Current Research in Pharmacology and Drug Discovery
                Elsevier
                2590-2571
                24 August 2023
                2023
                24 August 2023
                : 5
                : 100164
                Affiliations
                [1]Department of Chemistry, Durham University, Durham, DH1 3LE, United Kingdom
                Author notes
                []Corresponding author. exequiel.o.porta@ 123456durham.ac.uk
                Article
                S2590-2571(23)00012-3 100164
                10.1016/j.crphar.2023.100164
                10484978
                37692766
                b5925311-152c-4b91-8d25-7a5005026e25
                © 2023 The Authors

                This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).

                History
                : 17 April 2023
                : 6 August 2023
                : 23 August 2023
                Categories
                Article

                activity-based protein profiling,activity-based probes,affinity-based probes,chemical probes,chemoproteomics,drug discovery,mass spectrometry,target discovery

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