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Keywords = activography

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16 pages, 3848 KiB  
Review
Activity-Based Probes for Proteases Pave the Way to Theranostic Applications
by Georgia Sotiropoulou, Eleni Zingkou, Evangelos Bisyris and Georgios Pampalakis
Pharmaceutics 2022, 14(5), 977; https://doi.org/10.3390/pharmaceutics14050977 - 30 Apr 2022
Cited by 9 | Viewed by 2711
Abstract
Proteases are important enzymes in health and disease. Their activities are regulated at multiple levels. In fact, proteases are synthesized as inactive proenzymes (zymogens) that are activated by proteolytic removal of their pro-peptide sequence and can remain active or their activity can be [...] Read more.
Proteases are important enzymes in health and disease. Their activities are regulated at multiple levels. In fact, proteases are synthesized as inactive proenzymes (zymogens) that are activated by proteolytic removal of their pro-peptide sequence and can remain active or their activity can be attenuated by complex formation with specific endogenous inhibitors or by limited proteolysis or degradation. Consequently, quite often, only a fraction of the protease molecules is in the active/functional form, thus, the abundance of a protease is not always linearly proportional to the (patho)physiological function(s). Therefore, assays to determine the active forms of proteases are needed, not only in research but also in molecular diagnosis and therapy. Activity-based probes (ABPs) are chemical entities that bind covalently to the active enzyme/protease. ABPs carry a detection tag to enable localization and quantification of specific enzymatic/proteolytic activities with applications in molecular imaging and diagnosis. Moreover, ABPs act as suicide inhibitors of proteases, which can be exploited for delineation of the functional role(s) of a given protease in (patho) biological context and as potential therapeutics. In this sense, ABPs represent new theranostic agents. We outline recent developments pertaining to ABPs for proteases with potential therapeutic applications, with the aim to highlight their importance in theranostics. Full article
(This article belongs to the Special Issue New Advances in the Understanding of Proteases as Diagnostic and Pharmaceutical Targets in Homeostatic and Pathologic Conditions)
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