A novel theranostic activity-based probe targeting kallikrein 7 for the diagnosis and treatment of skin diseases

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Abstract

We applied a newin silicoapproach for using protease-substrate motifs to design a kallikrein 7 (KLK7)-specific phosphonate activity-based probe (ABP) to quantify the active KLK7in situ. Epidermal application of the ABP-inhibitor onSpink5−/−Klk5−/−mice, a Netherton syndrome model, reversed disease hallmarks, providing preclinical proof-of-concept for using ABPs as theranostics.

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Bisyris, E., Zingkou, E., Kordopati, G. G., Matsoukas, M., Magriotis, P. A., Pampalakis, G., & Sotiropoulou, G. (2021). A novel theranostic activity-based probe targeting kallikrein 7 for the diagnosis and treatment of skin diseases. Chemical Communications, 57(53), 6507–6510. https://doi.org/10.1039/d1cc01673c

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