Expanding the biological application of fluorescent benzothiadiazole derivatives: a phenotypic screening strategy for anthelmintic drug discovery using caenorhabditis elegans
Full metadata record
DC Field | Value | Language |
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dc.contributor.author | Cintra, Giovana A. S. | pt_BR |
dc.contributor.author | Neto, Brenno A. D. | pt_BR |
dc.contributor.author | Carvalho, Pedro H. P. R. | pt_BR |
dc.contributor.author | Moraes, Carolina Borsoi | pt_BR |
dc.contributor.author | Freitas-Junior, Lucio Holanda Gondim | pt_BR |
dc.date.accessioned | 2020-07-09T21:24:30Z | - |
dc.date.available | 2020-07-09T21:24:30Z | - |
dc.date.issued | 2019 | - |
dc.identifier.citation | Cintra 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.uri | https://repositorio.butantan.gov.br/handle/butantan/2787 | - |
dc.description.abstract | The 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.sponsorship | Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) | pt_BR |
dc.description.sponsorship | Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) | pt_BR |
dc.format.extent | p. 755-765 | pt_BR |
dc.language | eng | pt_BR |
dc.relation.ispartof | SLAS Discovery: Advancing the Science of Drug Discovery | pt_BR |
dc.rights | Open Access | pt_BR |
dc.title | Expanding the biological application of fluorescent benzothiadiazole derivatives | pt_BR |
dc.type | Article | pt_BR |
dc.identifier.doi | https://repositorio.butantan.gov.br/handle/butantan/2787 | pt_BR |
dc.identifier.url | https://doi.org/10.1177/2472555219851130 | pt_BR |
dc.contributor.external | Universidade de São Paulo (USP)¦¦Brasil | pt_BR |
dc.contributor.external | Centro Nacional de Pesquisa em Energia e Materiais (CNPEM)¦¦Brasil | pt_BR |
dc.contributor.external | Universidade de Brasília (UNB)¦¦Brasil | pt_BR |
dc.title.sub | a phenotypic screening strategy for anthelmintic drug discovery using caenorhabditis elegans | pt_BR |
dc.identifier.citationvolume | 24 | pt_BR |
dc.identifier.citationissue | 7 | pt_BR |
dc.subject.keyword | drug discovery | pt_BR |
dc.subject.keyword | Caenorhabditis elegans | pt_BR |
dc.subject.keyword | phenotypic screening | pt_BR |
dc.subject.keyword | benzothiadiazole derivatives | pt_BR |
dc.relation.ispartofabbreviated | SLAS Discov | pt_BR |
dc.identifier.citationabnt | v. 24, n. 7, p. 755-765, jun. 2019 | pt_BR |
dc.identifier.citationvancouver | 2019 June;24(7):755-765 | pt_BR |
dc.contributor.butantan | Cintra, Giovana A. S.|:Aluno|:|:PrimeiroAutor | pt_BR |
dc.contributor.butantan | Moraes, Carolina Borsoi|:Aluno|:|: | pt_BR |
dc.contributor.butantan | Freitas-Junior, Lucio Holanda Gondim|:Colaborador|:|: | pt_BR |
dc.sponsorship.butantan | Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)¦¦23038.006737/2012-56 | pt_BR |
dc.sponsorship.butantan | Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)¦¦2015/206326-7 | pt_BR |
dc.identifier.bvscc | BR78.1 | pt_BR |
dc.identifier.bvsdb | IBProd | pt_BR |
item.openairetype | Article | - |
item.fulltext | Com Texto completo | - |
item.grantfulltext | embargo_29990101 | - |
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crisitem.author.orcid | http://orcid.org/0000-0002-8904-7897 | - |
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crisitem.author.parentorg | #PLACEHOLDER_PARENT_METADATA_VALUE# | - |
Appears in Collections: | Artigos de periódicos |
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