The natural flavone fukugetin as a mixed-type inhibitor for human tissue kallikreins

The natural flavone fukugetin as a mixed-type inhibitor for human tissue kallikreins

Author Santos, Jorge A. N. Google Scholar
Kondo, Marcia Y. Autor UNIFESP Google Scholar
Freitas, Renato F. Google Scholar
dos Santos, Marcelo H. Google Scholar
Ramalho, Teodorico C. Google Scholar
Assis, Diego M. Autor UNIFESP Google Scholar
Juliano, Luiz Autor UNIFESP Google Scholar
Juliano, Maria A. Autor UNIFESP Google Scholar
Puzer, Luciano Google Scholar
Abstract The human tissue kallikreins (KLK1-KLK15) comprise a family of 15 serine peptidases detected in almost every tissue of the human body and that actively participate in many physiological and pathological events. Some kallikreins are involved in diseases for which no effective therapy is available, as for example, epithelial disorders, bacterial infections and in certain cancers metastatic processes. In recent years our group have made efforts to find inhibitors for all kallikreins, based on natural products and synthetic molecules, and all the inhibitors developed by our group presented a competitive mechanism of inhibition. Here we describe fukugetin, a natural product that presents a mixed-type mechanism of inhibition against KLK1 and KLK2. This type of inhibitor is gaining importance today, especially for the development of exosite-type inhibitors, which present potential to selectively inhibit the enzyme activity only against specific substrate. (C) 2016 Elsevier Ltd. All rights reserved.
Keywords Enzyme
Serine protease
Molecular docking
Molecular dynamic simulation
xmlui.dri2xhtml.METS-1.0.item-coverage Oxford
Language English
Sponsor Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP)
Grant number FAPESP: 2013/10548-3
Date 2016
Published in Bioorganic & Medicinal Chemistry Letters. Oxford, v. 26, n. 5, p. 1485-1489, 2016.
ISSN 0960-894X (Sherpa/Romeo, impact factor)
Publisher Pergamon-Elsevier Science Ltd
Extent 1485-1489
Access rights Closed access
Type Article
Web of Science ID WOS:000369941600024

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