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

Full metadata record
DC FieldValueLanguage
dc.contributor.authorCintra, Giovana Aparecida de Souzapt_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.issued2019pt_BR
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.language.isoEnglishpt_BR
dc.relation.ispartofSLAS Discovery: Advancing the Science of Drug Discoverypt_BR
dc.rightsOpen Accesspt_BR
dc.titleExpanding the biological application of fluorescent benzothiadiazole derivatives: a phenotypic screening strategy for anthelmintic drug discovery using caenorhabditis eleganspt_BR
dc.typeArticlept_BR
dc.identifier.doi10.1177/2472555219851130pt_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.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 Aparecida de Souza|: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
dc.description.dbindexedYespt_BR
item.openairetypeArticle-
item.fulltextCom Texto completo-
item.grantfulltextembargo_29990101-
item.languageiso639-1English-
crisitem.author.dept#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.author.dept#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.author.dept#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.author.dept#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.author.dept#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.author.orcid#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.author.orcid#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.author.orcid#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.author.orcid#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.author.orcid0000-0002-8904-7897-
crisitem.author.parentorg#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.author.parentorg#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.journal.journalissn#PLACEHOLDER_PARENT_METADATA_VALUE#-
crisitem.journal.journaleissn#PLACEHOLDER_PARENT_METADATA_VALUE#-
Appears in Collections:Artigos de periódicos


Files in This Item:

Existing users please Login
10.1177.2472555219851130.pdf
Size: 1.3 MB
Format: Adobe PDF
Embargoed until January 1, 2999    Request a copy
Show simple item record

The access to the publications deposited in this repository respects the licenses from journals and publishers.