Early toxicity screening and selection of lead compounds for parasitic diseases

Detalhes bibliográficos
Autor(a) principal: Nogueira, Renata Campos
Data de Publicação: 2009
Outros Autores: Costa, José Fernando Oliveira, Sá, Matheus Santos de, Santos, Ricardo Ribeiro dos, Soares, Milena Botelho Pereira
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/9009
Resumo: Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil
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spelling Nogueira, Renata CamposCosta, José Fernando OliveiraSá, Matheus Santos deSantos, Ricardo Ribeiro dosSoares, Milena Botelho Pereira2014-11-28T18:21:24Z2014-11-28T18:21:24Z2009NOGUEIRA, R. C. et al. Early toxicity screening and selection of lead compounds for parasitic diseases. Current Drug Targets, v. 10, n. 3, p. 291-298, 2009.1873-5592https://www.arca.fiocruz.br/handle/icict/9009engBentham Science Publishers LtdEarly toxicity screening and selection of lead compounds for parasitic diseasesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Salvador, BA, BrasilDespite many advances made in disease mechanisms knowledge and drug discovery and development processes, the election of promising lead compounds continues to be a challenge. Efficient techniques are required for lead selection of hit compounds selected through in vitro pharmacological studies, in order to generate precise low cost throughput data with minimal amount of compound to support the right decision making. In this context, the selection of lead compounds with physicochemical parameters that will benefit orally bioavailable drugs are crucial for patients compliance and cost effectiveness, as well as for successful pharmacology. A concept based in Lipinski’s rules point out the importance of analyzing these informations in early stages. A hepatocyte screening system may provide data on many processes such as drug-drug interaction, metabolite formation, drug toxicity and ADME profile of a hit. Drug-induced liver injury is the most frequent reason for the withdrawal of an approved drug from the market and hepatocytes have a central role in the metabolism of xenobiotics. Cytotoxicity screening assays can also give some information about toxicity early drug discovery process. A set of goals in lead compound selection must be shared between all areas involved so the chances of success can be improved in translational research.Toxicity screeningLead compoundParasitic diseasesDrug discoveryAntiparasitários/toxicidadeDesenho de DrogasDoenças Parasitárias/quimioterapiaAnimaisAntiparasitários/farmacocinéticaAntiparasitários/farmacologiaAvaliação Pré-Clínica de MedicamentosInterações de MedicamentosHepatócitos/efeitos de drogasHepatócitos/metabolismoHumanosTestes de Toxicidadeinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-81914https://www.arca.fiocruz.br/bitstream/icict/9009/1/license.txt7d48279ffeed55da8dfe2f8e81f3b81fMD51ORIGINALNogueira RC Early toxicity...pdfNogueira RC Early toxicity...pdfapplication/pdf194647https://www.arca.fiocruz.br/bitstream/icict/9009/2/Nogueira%20RC%20Early%20toxicity...pdf6c49a34105d1b2f97c9766bb437272d2MD52TEXTNogueira RC Early toxicity...pdf.txtNogueira RC Early toxicity...pdf.txtExtracted texttext/plain44636https://www.arca.fiocruz.br/bitstream/icict/9009/3/Nogueira%20RC%20Early%20toxicity...pdf.txt6aee20f4bfe7b4d4807aed070eba693aMD53icict/90092023-03-15 14:33:05.712oai:www.arca.fiocruz.br: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ório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352023-03-15T17:33:05Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv Early toxicity screening and selection of lead compounds for parasitic diseases
title Early toxicity screening and selection of lead compounds for parasitic diseases
spellingShingle Early toxicity screening and selection of lead compounds for parasitic diseases
Nogueira, Renata Campos
Toxicity screening
Lead compound
Parasitic diseases
Drug discovery
Antiparasitários/toxicidade
Desenho de Drogas
Doenças Parasitárias/quimioterapia
Animais
Antiparasitários/farmacocinética
Antiparasitários/farmacologia
Avaliação Pré-Clínica de Medicamentos
Interações de Medicamentos
Hepatócitos/efeitos de drogas
Hepatócitos/metabolismo
Humanos
Testes de Toxicidade
title_short Early toxicity screening and selection of lead compounds for parasitic diseases
title_full Early toxicity screening and selection of lead compounds for parasitic diseases
title_fullStr Early toxicity screening and selection of lead compounds for parasitic diseases
title_full_unstemmed Early toxicity screening and selection of lead compounds for parasitic diseases
title_sort Early toxicity screening and selection of lead compounds for parasitic diseases
author Nogueira, Renata Campos
author_facet Nogueira, Renata Campos
Costa, José Fernando Oliveira
Sá, Matheus Santos de
Santos, Ricardo Ribeiro dos
Soares, Milena Botelho Pereira
author_role author
author2 Costa, José Fernando Oliveira
Sá, Matheus Santos de
Santos, Ricardo Ribeiro dos
Soares, Milena Botelho Pereira
author2_role author
author
author
author
dc.contributor.author.fl_str_mv Nogueira, Renata Campos
Costa, José Fernando Oliveira
Sá, Matheus Santos de
Santos, Ricardo Ribeiro dos
Soares, Milena Botelho Pereira
dc.subject.en.pt_BR.fl_str_mv Toxicity screening
Lead compound
Parasitic diseases
Drug discovery
topic Toxicity screening
Lead compound
Parasitic diseases
Drug discovery
Antiparasitários/toxicidade
Desenho de Drogas
Doenças Parasitárias/quimioterapia
Animais
Antiparasitários/farmacocinética
Antiparasitários/farmacologia
Avaliação Pré-Clínica de Medicamentos
Interações de Medicamentos
Hepatócitos/efeitos de drogas
Hepatócitos/metabolismo
Humanos
Testes de Toxicidade
dc.subject.decs.pt_BR.fl_str_mv Antiparasitários/toxicidade
Desenho de Drogas
Doenças Parasitárias/quimioterapia
Animais
Antiparasitários/farmacocinética
Antiparasitários/farmacologia
Avaliação Pré-Clínica de Medicamentos
Interações de Medicamentos
Hepatócitos/efeitos de drogas
Hepatócitos/metabolismo
Humanos
Testes de Toxicidade
description Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil
publishDate 2009
dc.date.issued.fl_str_mv 2009
dc.date.accessioned.fl_str_mv 2014-11-28T18:21:24Z
dc.date.available.fl_str_mv 2014-11-28T18:21:24Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.citation.fl_str_mv NOGUEIRA, R. C. et al. Early toxicity screening and selection of lead compounds for parasitic diseases. Current Drug Targets, v. 10, n. 3, p. 291-298, 2009.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/9009
dc.identifier.issn.none.fl_str_mv 1873-5592
identifier_str_mv NOGUEIRA, R. C. et al. Early toxicity screening and selection of lead compounds for parasitic diseases. Current Drug Targets, v. 10, n. 3, p. 291-298, 2009.
1873-5592
url https://www.arca.fiocruz.br/handle/icict/9009
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Bentham Science Publishers Ltd
publisher.none.fl_str_mv Bentham Science Publishers Ltd
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
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