The natural flavone fukugetin as a mixed-type inhibitor for human tissue kallikreins.
Bioorg Med Chem Lett
; 26(5): 1485-9, 2016 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-26848109
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.
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Base de dados:
MEDLINE
Assunto principal:
Produtos Biológicos
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Inibidores de Serina Proteinase
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Calicreínas Teciduais
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Biflavonoides
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article