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Autor | Calvet, Claudia Magalhaes | |
Autor | Choi, Jun Yong | |
Autor | Thomas, Diane | |
Autor | Suzuki, Brian | |
Autor | Hirata, Ken | |
Autor | Lostracco-Johnson, Sharon | |
Autor | Mesquita, Liliane Batista de | |
Autor | Nogueira, Alanderson | |
Autor | Batista, Marcelo Meuser | |
Autor | Silva, Tatiana Araujo | |
Autor | Siqueira Neto, Jair Lage | |
Autor | Roush, William R. | |
Autor | Pereira, Mirian Claudia de Souza | |
Autor | McKerrow, James H. | |
Autor | Podust, Larissa M. | |
Fecha de acceso | 2018-02-08T10:38:50Z | |
Fecha de disponibilización | 2018-02-08T10:38:50Z | |
Fecha de publicación | 2017 | |
Referencia | CALVET, Claudia Magalhães et al. 4-aminopyridyl-based lead compounds targeting CYP51 prevent spontaneous parasite relapse in a chronic model and improve cardiac pathology in an acute model of Trypanosoma cruzi infection. PLOS Neglected Tropical Diseases, v.11, n.12, p. 1-12, Dec. 2017. | pt_BR |
ISSN | 1935-2727 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/24755 | |
Idioma | eng | pt_BR |
Editor | Public Library of Science | pt_BR |
Derechos de autor | open access | pt_BR |
Palabras clave en Portugués | Trypanosoma cruzi | pt_BR |
Palabras clave en Portugués | Doença de Chagas | pt_BR |
Palabras clave en Portugués | Tratamento | pt_BR |
Palabras clave en Portugués | Cardiomiopatias | pt_BR |
Palabras clave en Portugués | Infecção | pt_BR |
Título | 4-aminopyridyl-based lead compounds targeting CYP51 prevent spontaneous parasite relapse in a chronic model and improve cardiac pathology in an acute model of Trypanosoma cruzi infection | pt_BR |
Tipo del documento | Article | pt_BR |
DOI | 10.1371/journal.pntd.0006132 | |
Resumen en Inglés | Chagas disease, caused by the protozoan Trypanosoma cruzi, is the leading cause of heart failure in Latin America. The clinical treatment of Chagas disease is limited to two 60 year-old drugs, nifurtimox and benznidazole, that have variable efficacy against different strains of the parasite and may lead to severe side effects. CYP51 is an enzyme in the sterol biosynthesis pathway that has been exploited for the development of therapeutics for fungal and parasitic infections. In a target-based drug discovery program guided by x-ray crystallography, we identified the 4-aminopyridyl-based series of CYP51 inhibitors as being efficacious versus T.cruzi in vitro; two of the most potent leads, 9 and 12, have now been evaluated for toxicity and efficacy in mice. | pt_BR |
Afiliación | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. La Jolla. Center for Discovery and Innovation in Parasitic Diseases. CA, USA / Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Ultraestrutura Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
Afiliación | Scripps Florida. Department of Chemistry. Jupiter, Florida, USA. | pt_BR |
Afiliación | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. La Jolla. Center for Discovery and Innovation in Parasitic Diseases. CA, USA. | pt_BR |
Afiliación | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. La Jolla. Center for Discovery and Innovation in Parasitic Diseases. CA, USA. | pt_BR |
Afiliación | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. La Jolla. Center for Discovery and Innovation in Parasitic Diseases. CA, USA. | pt_BR |
Afiliación | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. La Jolla. Center for Discovery and Innovation in Parasitic Diseases. CA, USA. | pt_BR |
Afiliación | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Ultraestrutura Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
Afiliación | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Ultraestrutura Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
Afiliación | Fundação Oswaldo Cruz. Instituto Fernandes Figueira. Departamento de Anatomia Patológica. Rio de Janeiro, RJ. Brasil . | pt_BR |
Afiliación | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Ultraestrutura Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
Afiliación | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. La Jolla. Center for Discovery and Innovation in Parasitic Diseases. CA, USA. | pt_BR |
Afiliación | Scripps Florida. Department of Chemistry. Jupiter, Florida, USA. | pt_BR |
Afiliación | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Ultraestrutura Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
Afiliación | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. La Jolla. Center for Discovery and Innovation in Parasitic Diseases. CA, USA. | pt_BR |
Afiliación | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. La Jolla. Center for Discovery and Innovation in Parasitic Diseases. CA, USA. | pt_BR |
Palavras clave en Inglês | Trypanosoma cruzi | pt_BR |
Palavras clave en Inglês | Chagas Disease | pt_BR |
Palavras clave en Inglês | Treatment | pt_BR |
Palavras clave en Inglês | Cardiomiopathy | pt_BR |
Palavras clave en Inglês | Infection | pt_BR |
e-ISSN | 1935-2735 |
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