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

Show simple item record 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 2018-05-18T12:17:21Z 2018-05-18T12:17:21Z 2016-03-01
dc.identifier.issn 0960894X
dc.description.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. en
dc.format pdf pt-BR
dc.language.iso eng pt-BR
dc.publisher Bioorganic & Medicinal Chemistry Letters pt-BR
dc.relation.ispartofseries v. 26, n. 5, p. 1485-1489, Março 2016 pt-BR
dc.rights Elsevier Ltd pt-BR
dc.subject Enzyme pt-BR
dc.subject Serine protease pt-BR
dc.subject Kallikrein pt-BR
dc.subject Inhibitor pt-BR
dc.subject Flavone pt-BR
dc.subject Molecular docking pt-BR
dc.subject Molecular dynamic simulation pt-BR
dc.title The natural flavone fukugetin as a mixed-type inhibitor for human tissue kallikreins en
dc.type Artigo pt-BR

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    Artigos Técnico-científicos na área de Química

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