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| Mottin,Melina; Borba,Joyce Villa Verde Bastos; Melo-Filho,Cleber Camilo; Neves,Bruno Junior; Muratov,Eugene; Torres,Pedro Henrique Monteiro; Braga,Rodolpho Campos; Perryman,Alexander; Ekins,Sean; Andrade,Carolina Horta. |
| Few Zika virus (ZIKV) outbreaks had been reported since its first detection in 1947, until the recent epidemics occurred in South America (2014/2015) and expeditiously became a global public health emergency. This arbovirus reached 0.5-1.3 million cases of ZIKV infection in Brazil in 2015 and rapidly spread in new geographic areas such as the Americas. Despite the mild symptoms of the Zika fever, the major concern is related to the related severe neurological disorders, especially microcephaly in newborns. Advances in ZIKV drug discovery have been made recently and constitute promising approaches to ZIKV treatment. In this review, we summarize current computational drug discovery efforts and their applicability to discovery of anti-ZIKV drugs. Lastly, we... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Zika; Flavivirus Antiviral; Computer-assisted drug design; Virtual screening; Drug discovery. |
| Ano: 2018 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502018000700401 |
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| Ferreira,Daiane Dias; Mesquita,Juliana Tonini; Silva,Thais Alves da Costa; Romanelli,Maiara Maria; Batista,Denise da Gama Jaen; Silva,Cristiane França da; Gama,Aline Nefertiti Silva da; Neves,Bruno Junior; Melo-Filho,Cleber Camilo; Soeiro,Maria de Nazare Correia; Andrade,Carolina Horta; Tempone,Andre Gustavo. |
| Abstract Background: Drug repurposing has been an interesting and cost-effective approach, especially for neglected diseases, such as Chagas disease. Methods: In this work, we studied the activity of the antidepressant drug sertraline against Trypanosoma cruzi trypomastigotes and intracellular amastigotes of the Y and Tulahuen strains, and investigated its action mode using cell biology and in silico approaches. Results: Sertraline demonstrated in vitro efficacy against intracellular amastigotes of both T. cruzi strains inside different host cells, including cardiomyocytes, with IC50 values between 1 to 10 μM, and activity against bloodstream trypomastigotes, with IC50 of 14 μM. Considering the mammalian cytotoxicity, the drug resulted in a selectivity... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Trypanosoma cruzi; Drug; Treatment; Sertraline; Drug repurposing; Drug repositioning. |
| Ano: 2018 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1678-91992018000100321 |
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