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

Página do item simplificado
dc.citation.issue5
dc.citation.volume26
dc.contributor.authorSantos, Jorge A. N.
dc.contributor.authorKondo, Marcia Y. [UNIFESP]
dc.contributor.authorFreitas, Renato F.
dc.contributor.authordos Santos, Marcelo H.
dc.contributor.authorRamalho, Teodorico C.
dc.contributor.authorAssis, Diego M. [UNIFESP]
dc.contributor.authorJuliano, Luiz [UNIFESP]
dc.contributor.authorJuliano, Maria A. [UNIFESP]
dc.contributor.authorPuzer, Luciano
dc.coverageOxford
dc.date.accessioned2020-08-21T17:00:18Z
dc.date.available2020-08-21T17:00:18Z
dc.date.issued2016
dc.description.abstractThe 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.en
dc.description.affiliationInst Fed Ciencia Tecnol & Educ Sul Minas Gerais, Belo Horizonte, MG, Brazil
dc.description.affiliationUniv Fed Sao Paulo, Dept Biofis, Sao Paulo, SP, Brazil
dc.description.affiliationJohns Hopkins Univ, Dept Biol, Baltimore, MD 21218 USA
dc.description.affiliationUniv Fed Vicosa, Dept Quim, Vicosa, MG, Brazil
dc.description.affiliationUniv Fed Lavras, Dept Quim, Lavras, MG, Brazil
dc.description.affiliationUniv Fed ABC, Ctr Ciencias Nat & Humanas, BR-09606070 Sao Bernardo Do Campo, SP, Brazil
dc.description.affiliationUnifespUniv Fed Sao Paulo, Dept Biofis, Sao Paulo, SP, Brazil
dc.description.sourceWeb of Science
dc.description.sponsorshipFundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP)
dc.description.sponsorshipIDFAPESP: 2013/10548-3
dc.format.extent1485-1489
dc.identifierhttp://dx.doi.org/10.1016/j.bmcl.2016.01.039
dc.identifier.citationBioorganic & Medicinal Chemistry Letters. Oxford, v. 26, n. 5, p. 1485-1489, 2016.
dc.identifier.doi10.1016/j.bmcl.2016.01.039
dc.identifier.issn0960-894X
dc.identifier.urihttps://repositorio.unifesp.br/handle/11600/57934
dc.identifier.wosWOS:000369941600024
dc.language.isoeng
dc.publisherPergamon-Elsevier Science Ltd
dc.relation.ispartofBioorganic & Medicinal Chemistry Letters
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.subjectEnzymeen
dc.subjectSerine proteaseen
dc.subjectKallikreinen
dc.subjectInhibitoren
dc.subjectFlavoneen
dc.subjectMolecular dockingen
dc.subjectMolecular dynamic simulationen
dc.titleThe natural flavone fukugetin as a mixed-type inhibitor for human tissue kallikreinsen
dc.typeinfo:eu-repo/semantics/article
Arquivos
Coleções
EPM - Artigos