Expanding the biological application of fluorescent benzothiadiazole derivatives: a phenotypic screening strategy for anthelmintic drug discovery using caenorhabditis elegans

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dc.contributor.authorCintra, Giovana A. S.pt_BR
dc.contributor.authorNeto, Brenno A. D.pt_BR
dc.contributor.authorCarvalho, Pedro H. P. R.pt_BR
dc.contributor.authorMoraes, Carolina Borsoipt_BR
dc.contributor.authorFreitas-Junior, Lucio Holanda Gondimpt_BR
dc.date.accessioned2020-07-09T21:24:30Z-
dc.date.available2020-07-09T21:24:30Z-
dc.date.issued2019-
dc.identifier.citationCintra GA.S., Neto BA.D., Carvalho PH.P.R., Moraes CB, Freitas-Junior LHG. Expanding the biological application of fluorescent benzothiadiazole derivatives: a phenotypic screening strategy for anthelmintic drug discovery using caenorhabditis elegans. SLAS Discov. 2019 June;24(7):755-765. doi:doi.org/10.1177/2472555219851130.pt_BR
dc.identifier.urihttps://repositorio.butantan.gov.br/handle/butantan/2787-
dc.description.abstractThe current methodologies used to identify promising new anthelmintic compounds rely on subjective microscopic examination of worm motility or involve genetic modified organisms. We describe a new methodology to detect worm viability that takes advantage of the differential incorporation of the fluorescent molecular marker propidium iodide and the 2,1,3-benzothiadiazole core, which has been widely applied in light technology. The new assay developed could be validated using the "Pathogen Box" library. By use of this bioassay, it was possible to identify three molecules with activity against Caenorhabditis elegans that were previously described as effective in in vitro assays against other pathogens, such as Schistosoma mansoni, Mycobacterium tuberculosis, and Plasmodium falciparum, accelerating the identification of molecules with anthelmintic potential. The current fluorescence-based bioassay may be used for assessing C. elegans viability. The described methodology replaces the subjectivity of previous assays and provides an enabling technology that is useful for rapid in vitro screens of both natural and synthetic compound libraries. It is expected that the results obtained from these robust in vitro screens would select the most effective compounds for follow-up in vivo experimentation with pathogenic helminths.pt_BR
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)pt_BR
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)pt_BR
dc.format.extentp. 755-765pt_BR
dc.languageengpt_BR
dc.relation.ispartofSLAS Discovery: Advancing the Science of Drug Discoverypt_BR
dc.rightsOpen Accesspt_BR
dc.titleExpanding the biological application of fluorescent benzothiadiazole derivativespt_BR
dc.typeArticlept_BR
dc.identifier.doihttps://repositorio.butantan.gov.br/handle/butantan/2787pt_BR
dc.identifier.urlhttps://doi.org/10.1177/2472555219851130pt_BR
dc.contributor.externalUniversidade de São Paulo (USP)¦¦Brasilpt_BR
dc.contributor.externalCentro Nacional de Pesquisa em Energia e Materiais (CNPEM)¦¦Brasilpt_BR
dc.contributor.externalUniversidade de Brasília (UNB)¦¦Brasilpt_BR
dc.title.suba phenotypic screening strategy for anthelmintic drug discovery using caenorhabditis eleganspt_BR
dc.identifier.citationvolume24pt_BR
dc.identifier.citationissue7pt_BR
dc.subject.keyworddrug discoverypt_BR
dc.subject.keywordCaenorhabditis eleganspt_BR
dc.subject.keywordphenotypic screeningpt_BR
dc.subject.keywordbenzothiadiazole derivativespt_BR
dc.relation.ispartofabbreviatedSLAS Discovpt_BR
dc.identifier.citationabntv. 24, n. 7, p. 755-765, jun. 2019pt_BR
dc.identifier.citationvancouver2019 June;24(7):755-765pt_BR
dc.contributor.butantanCintra, Giovana A. S.|:Aluno|:|:PrimeiroAutorpt_BR
dc.contributor.butantanMoraes, Carolina Borsoi|:Aluno|:|:pt_BR
dc.contributor.butantanFreitas-Junior, Lucio Holanda Gondim|:Colaborador|:|:pt_BR
dc.sponsorship.butantanCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)¦¦23038.006737/2012-56pt_BR
dc.sponsorship.butantanFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)¦¦2015/206326-7pt_BR
dc.identifier.bvsccBR78.1pt_BR
dc.identifier.bvsdbIBProdpt_BR
item.openairetypeArticle-
item.fulltextCom Texto completo-
item.grantfulltextembargo_29990101-
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