A novel theranostic activity-based probe targeting kallikrein 7 for the diagnosis and treatment of skin diseases†
Golfo G.
Kordopati, 
a
Minos
Matsoukas,
a
Plato A.
Magriotis,
a
Georgios
Pampalakis
‡*a
and
Georgia
Sotiropoulou
*a
a
Minos
Matsoukas,
a
Plato A.
Magriotis,
a
Georgios
Pampalakis
‡*a
and
Georgia
Sotiropoulou
*a
Abstract
We applied a new in silico approach for using protease-substrate motifs to design a kallikrein 7 (KLK7)-specific phosphonate activity-based probe (ABP) to quantify the active KLK7 in situ. Epidermal application of the ABP-inhibitor on Spink5−/−Klk5−/− mice, a Netherton syndrome model, reversed disease hallmarks, providing preclinical proof-of-concept for using ABPs as theranostics.
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