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Bioorg Med Chem Lett. 2013 Aug 15;23(16):4547-51. doi: 10.1016/j.bmcl.2013.06.039. Epub 2013 Jun 24.

1,2,4-Triazole derivatives as transient inactivators of kallikreins involved in skin diseases.

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  • 1Enzymologie Moléculaire et Fonctionnelle, UR4, Université Pierre et Marie Curie-Sorbonne Universités (UPMC), Case Courrier 256, 7, Quai St Bernard, 75252 Paris Cedex 05, France.


We describe here 1,2,4-triazoles derivatives identified as transient inactivators acting at the nanomolar level on human kallikreins (hK5, hK7 and hK14) and matriptase. Both the nature of the targeted enzymes and structural variations of the inhibitors influence the life-times of acyl-enzymes. These nonpeptidic, transient and low-molecular-weight inhibitors were found to be noncytotoxic against healthy human keratinocytes. These molecules may be useful to counteract dysregulated proteolytic cascades observed in dermatological disorders such as Netherton syndrome.

Copyright © 2013 Elsevier Ltd. All rights reserved.


3-amino-7-methyl-coumarin; AMC; Acyl-enzymes; DMSO; HTS; Inhibitors; Kallikreins; LEKTI; Matriptase; Netherton syndrome; Transient inactivators; dimethyl sulfoxide; hK; high throughput screening; human kallikrein; lympho-epithelial Kazal-type inhibitor

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