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Serine proteases are one of the largest mechanistic classes of proteases. They regulate a plethora of biochemical pathways inside and outside the cell. Aberrant serine protease activity leads to a wide variety of human diseases. Reagents to visualize these activities can be used to gain insight into the biological roles of serine proteases. Moreover, they may find future use for the detection of serine proteases as biomarkers. In this review, we discuss small molecule tools to image serine protease activity. Specifically, we outline different covalent activity-based probes and their selectivity against various serine protease targets. We also describe their application in several imaging methods. © 2024 The Author(s). Published by Portland Press Limited on behalf of the Biochemical Society.

Citation

Marcin Skorenski, Shanping Ji, Steven H L Verhelst. Covalent activity-based probes for imaging of serine proteases. Biochemical Society transactions. 2024 Apr 24;52(2):923-935

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PMID: 38629725

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