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Small-molecule probes elucidate global enzyme activity in a proteomic context

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The recent dramatic improvements in high-resolution massspectrometry (MS) have revolutionized the speed and scope ofproteomic studies. Conventional MS-based proteomicsmethodologies allow global protein profiling based onexpression levels. Although these techniques are promising,there are numerous biological activities yet to be unveiled,such as the dynamic regulation of enzyme activity. Chemicalproteomics is an emerging field that extends these typesproteomic profiling. In particular, activity-based proteinprofiling (ABPP) utilizes small-molecule probes to monitorenzyme activity directly in living intact subjects. In thismini-review, we summarize the unique roles of smallmoleculeprobes in proteomics studies and highlight somerecent examples in which this principle has been applied.

Abstract

The recent dramatic improvements in high-resolution massspectrometry (MS) have revolutionized the speed and scope ofproteomic studies. Conventional MS-based proteomicsmethodologies allow global protein profiling based onexpression levels. Although these techniques are promising,there are numerous biological activities yet to be unveiled,such as the dynamic regulation of enzyme activity. Chemicalproteomics is an emerging field that extends these typesproteomic profiling. In particular, activity-based proteinprofiling (ABPP) utilizes small-molecule probes to monitorenzyme activity directly in living intact subjects. In thismini-review, we summarize the unique roles of smallmoleculeprobes in proteomics studies and highlight somerecent examples in which this principle has been applied.

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