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Use este identificador para citar ou linkar para este item: https://repositorio.ufba.br/handle/ri/20742
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dc.contributor.authorOliveira, Diêgo Madureira de-
dc.contributor.authorFarias, Marcel Tavares de-
dc.contributor.authorTeles, André Lacerda Braga-
dc.contributor.authorSantos Junior, Manoelito Coelho dos-
dc.contributor.authorCerqueira, Martins Dias de-
dc.contributor.authorLima, Rute Maria Ferreira-
dc.contributor.authorEl-Bachá, Ramon dos Santos-
dc.creatorOliveira, Diêgo Madureira de-
dc.creatorFarias, Marcel Tavares de-
dc.creatorTeles, André Lacerda Braga-
dc.creatorSantos Junior, Manoelito Coelho dos-
dc.creatorCerqueira, Martins Dias de-
dc.creatorLima, Rute Maria Ferreira-
dc.creatorEl-Bachá, Ramon dos Santos-
dc.date.accessioned2016-10-06T13:28:03Z-
dc.date.available2016-10-06T13:28:03Z-
dc.date.issued2014-09-30-
dc.identifier.citationOliveira, et al... 2014pt_BR
dc.identifier.issn1664-8714-
dc.identifier.urihttp://repositorio.ufba.br/ri/handle/ri/20742-
dc.description.abstractThe blood-brain barrier (BBB) is known to protect healthy brain cells from potentially dangerous chemical agents, but there are many evidences supporting the idea that this protective action is extended to tumor cells. Since the process of angiogenesis in brain tumors leads to BBB breakdown, biochemical characteristics of the BBB seem to be more relevant than physical barriers to protect tumor cells from chemotherapy. In fact, a number of resistance related factors were already demonstrated to be component of both BBB and tumor cells. The enzyme glutathione S-transferases (GST) detoxify electrophilic xenobiotics and endogenous secondary metabolites formed during oxidative stress. A role has been attributed to GST in the resistance of cancer cells to chemotherapeutic agents. This study characterized 8-methoxypsoralen (8-MOP) as a human GST P1-1 (hGST P1-1) inhibitor. To identify and characterize the potential inhibitory activity of 8-MOP, we studied the enzyme kinetics of the conjugation of 1-chloro-2,4-dinitrobenzene (CDNB) with GSH catalyzed by hGST P1-1. We report here that 8-MOP competitively inhibited hGST P1-1 relative to CDNB, but there was an uncompetitive inhibition relative to GSH. Chromatographic analyses suggest that 8-MOP is not a substrate. Molecular docking simulations suggest that 8-MOP binds to the active site, but its position prevents the GSH conjugation. Thus, we conclude that 8-MOP is a promising prototype for new GST inhibitors pharmacologically useful in the treatment of neurodegenerative disorders and the resistance of cancer to chemotherapy.pt_BR
dc.description.sponsorshipCNPq/BNBpt_BR
dc.language.isoenpt_BR
dc.publisherFrontiers in Cellular Neurosciencept_BR
dc.rightsAcesso Abertopt_BR
dc.sourcehttp://journal.frontiersin.org/article/10.3389/fncel.2014.00308/fullpt_BR
dc.subjectGSTpt_BR
dc.subject8-MOPpt_BR
dc.subjectglioblastomapt_BR
dc.title8-Methoxypsoralen is a competitive inhibitor of glutathioneS-transferase P1-1pt_BR
dc.typeArtigo de Periódicopt_BR
dc.identifier.numberV. 8pt_BR
dc.publisher.countryBrasilpt_BR
Aparece nas coleções:Artigo Publicado em Periódico (ICS)

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