Activity-based proteomics: enzymatic activity profiling in complex proteomes |
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Authors: | H Schmidinger A Hermetter R Birner-Gruenberger |
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Institution: | (1) Department of Biochemistry, Graz University of Technology, Graz, Austria |
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Abstract: | Summary. In the postgenomic era new technologies are emerging for global analysis of protein function. The introduction of active site-directed
chemical probes for enzymatic activity profiling in complex mixtures, known as activity-based proteomics has greatly accelerated
functional annotation of proteins. Here we review probe design for different enzyme classes including serine hydrolases, cysteine
proteases, tyrosine phosphatases, glycosidases, and others. These probes are usually detected by their fluorescent, radioactive
or affinity tags and their protein targets are analyzed using established proteomics techniques. Recent developments, such
as the design of probes for in vivo analysis of proteomes, as well as microarray technologies for higher throughput screenings
of protein specificity and the application of activity-based probes for drug screening are highlighted. We focus on biological
applications of activity-based probes for target and inhibitor discovery and discuss challenges for future development of
this field. |
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Keywords: | : Activity-based proteomics – Functional proteomics – Enzymatic activity profiling – Active site-directed chemical probes |
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