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A novel theranostic activity-based probe targeting kallikrein 7 for the diagnosis and treatment of skin diseases.
Bisyris, Evangelos; Zingkou, Eleni; Kordopati, Golfo G; Matsoukas, Minos; Magriotis, Plato A; Pampalakis, Georgios; Sotiropoulou, Georgia.
Afiliação
  • Bisyris E; Department of Pharmacy, School of Health Sciences, University of Patras, Rion-Patras, 26504, Greece. gpampalakis@pharm.auth.gr gdsotiro@upatras.gr.
  • Zingkou E; Department of Pharmacy, School of Health Sciences, University of Patras, Rion-Patras, 26504, Greece. gpampalakis@pharm.auth.gr gdsotiro@upatras.gr.
  • Kordopati GG; Department of Pharmacy, School of Health Sciences, University of Patras, Rion-Patras, 26504, Greece. gpampalakis@pharm.auth.gr gdsotiro@upatras.gr.
  • Matsoukas M; Department of Pharmacy, School of Health Sciences, University of Patras, Rion-Patras, 26504, Greece. gpampalakis@pharm.auth.gr gdsotiro@upatras.gr.
  • Magriotis PA; Department of Pharmacy, School of Health Sciences, University of Patras, Rion-Patras, 26504, Greece. gpampalakis@pharm.auth.gr gdsotiro@upatras.gr.
  • Pampalakis G; Department of Pharmacy, School of Health Sciences, University of Patras, Rion-Patras, 26504, Greece. gpampalakis@pharm.auth.gr gdsotiro@upatras.gr.
  • Sotiropoulou G; Department of Pharmacy, School of Health Sciences, University of Patras, Rion-Patras, 26504, Greece. gpampalakis@pharm.auth.gr gdsotiro@upatras.gr.
Chem Commun (Camb) ; 57(53): 6507-6510, 2021 Jul 07.
Article em En | MEDLINE | ID: mdl-34105530
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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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Dermatopatias / Simulação por Computador / Calicreínas / Sondas Moleculares Idioma: En Ano de publicação: 2021 Tipo de documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Dermatopatias / Simulação por Computador / Calicreínas / Sondas Moleculares Idioma: En Ano de publicação: 2021 Tipo de documento: Article