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3-Cyano-3-aza-β-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins

  • Nitrile-type inhibitors are known to interact with cysteine proteases in a covalent-reversible manner. The chemotype of 3-cyano-3-aza-β-amino acid derivatives was designed in which the N-cyano group is centrally arranged in the molecule to allow for interactions with the nonprimed and primed binding regions of the target enzymes. These compounds were evaluated as inhibitors of the human cysteine cathepsins K, S, B, and L. They exhibited slow-binding behavior and were found to be exceptionally potent, in particular toward cathepsin K, with second-order rate constants up to 52 900 × 103 M–1 s–1.

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Document Type:Article
Author:Janina Schmitz, Anna-Madeleine Beckmann, Adela Dudic, Tianwei Li, Robert Sellier, Ulrike Bartz, Michael Gütschow
Parent Title (English):ACS Medicinal Chemistry Letters
First Page:1076
Last Page:1081
Pubmed Id:http://www.ncbi.nlm.nih.gov/pubmed?term=25313316
Publisher:ACS Publications
Publishing Institution:Hochschule Bonn-Rhein-Sieg
Date of first publication:2014/09/03
Tag:cysteine proteases; human cathepsins; nitrile inhibitors; β-amino acids
Departments, institutes and facilities:Fachbereich Angewandte Naturwissenschaften
Dewey Decimal Classification (DDC):6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit
Entry in this database:2015/04/02
Licence (English):License LogoACS AuthorChoice/Editors’ Choice License