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https://locus.ufv.br//handle/123456789/19688
Tipo: | Artigo |
Título: | The natural flavone fukugetin as a mixed-type inhibitor for human tissue kallikreins |
Autor(es): | Santos, Marcelo H. dos Santos, Jorge A. N. Kondo, Márcia Y. Freitas, Renato F. Ramalho, Teodorico C. Assis, Diego M. Juliano, Luiz Juliano, Maria A. Puzer, Luciano |
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. |
Palavras-chave: | Enzyme Serine protease Kallikrein Inhibitor Flavone Molecular docking Molecular dynamic simulation |
Editor: | Bioorganic & Medicinal Chemistry Letters |
Tipo de Acesso: | Elsevier Ltd |
URI: | https://doi.org/10.1016/j.bmcl.2016.01.039 http://www.locus.ufv.br/handle/123456789/19688 |
Data do documento: | 1-Mar-2016 |
Aparece nas coleções: | Artigos |
Arquivos associados a este item:
Arquivo | Descrição | Tamanho | Formato | |
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artigo.pdf Until 2100-12-31 | texto completo | 1,05 MB | Adobe PDF | Visualizar/Abrir ACESSO RESTRITO |
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