Phage Display Selected Cyclic Peptide Inhibitors of Kallikrein-Related Peptidases 5 and 7 and Their


Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
28 07 2022
Historique:
pubmed: 3 6 2022
medline: 30 7 2022
entrez: 2 6 2022
Statut: ppublish

Résumé

Kallikrein-related peptidases 5 (KLK5) and 7 (KLK7) are serine proteases with homeostatic functions in the epidermis that play a critical role in Netherton syndrome (NS), a rare yet life-threatening genetic disorder that currently lacks specific treatment. Previous research suggests that controlling KLKs could lead to the development of NS therapies, but existing synthetic inhibitors have limitations. Herein, we used phage display to screen libraries comprising more than 100 billion different cyclic peptides and found selective, high-affinity inhibitors of KLK5 (

Identifiants

pubmed: 35653695
doi: 10.1021/acs.jmedchem.2c00306
doi:

Substances chimiques

Peptides 0
Peptides, Cyclic 0
Kallikreins EC 3.4.21.-

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

9735-9749

Auteurs

Patrick Gonschorek (P)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Alessandro Zorzi (A)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Tamara Maric (T)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Mathilde Le Jeune (M)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Mischa Schüttel (M)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Mathilde Montagnon (M)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Rebeca Gómez-Ojea (R)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Denis Patrick Vollmar (DP)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Chantal Whitfield (C)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Luc Reymond (L)

Biomolecular Screening Facility, Swiss Federal Institute of Technology Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Vanessa Carle (V)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Hitesh Verma (H)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

Oliver Schilling (O)

Institute for Surgical Pathology, Medical Center, Faculty of Medicine, University of Freiburg, Freiburg 79106, Germany.

Alain Hovnanian (A)

INSERM UMR1163, Imagine Institute, University of Paris, Paris, France; Department of Genetics, Necker Hospital for Sick Children (AP-HP), 75015 Paris, France.

Christian Heinis (C)

Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne CH-1015, Switzerland.

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Classifications MeSH