Journal ArticleDOI
Identification and characterization of Zika virus NS5 RNA-dependent RNA polymerase inhibitors.
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TLDR
A fluorescence-based polymerase assay is used to find an anti-infective drug 10-undecenoic acid zinc salt (UA), which could inhibit RdRp activity with an IC50 of 1.13-1.25 μM and shows anti-ZIKV activity comparable to sofosbuvir.About:
This article is published in International Journal of Antimicrobial Agents.The article was published on 2019-07-13. It has received 28 citations till now. The article focuses on the topics: RNA-dependent RNA polymerase & Polymerase.read more
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A promising antiviral candidate drug for the COVID-19 pandemic: A mini-review of remdesivir.
Liang Chengyuan,Lei Tian,Liu Yuzhi,Hui Nan,Qiao Guaiping,Li Han,Zhenfeng Shi,Tang Yonghong,Zhang Dezhu,Xie Xiaolin,Xu Zhao +10 more
TL;DR: This review presents comprehensive information on remdesivir, including information regarding the milestones, intellectual properties, anti-coronavirus mechanisms, preclinical research and clinical trials, and in particular, the chemical synthesis, pharmacology, toxicology, pharmacodynamics and pharmacokinetics of remdesvir.
Journal ArticleDOI
Antiviral activity of lycorine against Zika virus in vivo and in vitro.
Huini Chen,Zizhao Lao,Jiangtao Xu,Zhaoxin Li,Haishan Long,Detang Li,Luping Lin,Xiaohong Liu,Yu Liangwen,Weiyong Liu,Geng Li,Geng Li,Jianguo Wu +12 more
TL;DR: Lycorine protected AG6 mice against ZIKV-induced lethality by decreasing the viral load in the blood and might offer promising therapeutic possibilities for combatting ZikV infections in the future.
Journal Article
Zika Virus NS5 Protein Potential Inhibitors: An Enhanced in silico Approach in Drug Discovery
TL;DR: In this article, an optimized and proven screening technique was used in the discovery of two potential small molecule inhibitors of ZIKV Methyltransferase and RNA dependent RNA polymerase.
Journal ArticleDOI
Non-nucleoside Inhibitors of Zika Virus RNA-Dependent RNA Polymerase.
Aïcha Gharbi-Ayachi,Sridhar Santhanakrishnan,Yee Hwa Wong,Kitti Wing Ki Chan,Siok Thing Tan,Roderick W. Bates,Subhash G. Vasudevan,Subhash G. Vasudevan,Abbas El Sahili,Julien Lescar +9 more
TL;DR: The development of small nonnucleoside inhibitors (NNIs) of ZIKV RNA-dependent RNA polymerase (RdRp) activity target an allosteric pocket (N pocket) located next to a putative hinge region between the thumb and the palm subdomains that was originally described for dengue virus (DENV) RdRp.
Journal ArticleDOI
Importance of Zika Virus NS5 Protein for Viral Replication.
TL;DR: Zika virus is the latest addition to an ever-growing list of arboviruses that are causing outbreaks with serious consequences, however, recent studies have taken interest in the NS5 protein which encodes both the viral methyltransferase and RNA-dependent RNA polymerase.
References
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Journal ArticleDOI
Chloroquine, an Endocytosis Blocking Agent, Inhibits Zika Virus Infection in Different Cell Models
Rodrigo Delvecchio,Luisa M. Higa,Paula Pezzuto,Ana Luiza Chaves Valadão,Patricia P. Garcez,Fábio Luiz Monteiro,Erick Correia Loiola,André Alves Dias,Fabio J Moreira da Silva,Matthew T. Aliota,Elizabeth A. Caine,Jorge E. Osorio,Maria Bellio,David H. O’Connor,Stevens K. Rehen,Renato S. Aguiar,Andrea Savarino,Loraine Campanati,Amilcar Tanuri +18 more
TL;DR: It is demonstrated that chloroquine reduces the number of ZikV-infected cells in vitro, and inhibits virus production and cell death promoted by ZIKV infection without cytotoxic effects.
Journal ArticleDOI
The clinically approved antiviral drug sofosbuvir inhibits Zika virus replication
Carolina Q. Sacramento,Gabrielle R. de Melo,Caroline S. de Freitas,Natasha Rocha,Lucas Villas Bôas Hoelz,Milene D. Miranda,Milene D. Miranda,Natalia Fintelman-Rodrigues,Andressa Marttorelli,André C. Ferreira,Giselle Barbosa-Lima,Juliana L. Abrantes,Juliana L. Abrantes,Yasmine Rangel Vieira,Mônica M. Bastos,Eduardo de Mello Volotão,Estevão Portela Nunes,Diogo A. Tschoeke,Diogo A. Tschoeke,Luciana Leomil,Luciana Leomil,Erick Correia Loiola,Pablo Trindade,Stevens K. Rehen,Fernando A. Bozza,Patrícia T. Bozza,Nubia Boechat,Fabiano L. Thompson,Fabiano L. Thompson,Ana M. B. de Filippis,Karin Brüning,Thiago Moreno L. Souza +31 more
TL;DR: Sofosbuvir inhibited ZIKV replication in different cellular systems, such as hepatoma (Huh-7) cells, neuroblastoma (SH-Sy5y), neural stem cells (NSC) and brain organoids, and induced an increase in A-to-G mutations in the viral genome, highlighting a potential secondary use of sofosBuvir, an anti-HCV drug, against ZikV.
Journal ArticleDOI
Structure and Function of the Zika Virus Full-Length NS5 Protein
Baoyu Zhao,Guanghui Yi,Fenglei Du,Yin Chih Chuang,Robert C. Vaughan,Banumathi Sankaran,C. Cheng Kao,Pingwei Li +7 more
TL;DR: The crystal structures of full-length NS5 and its polymerase domain at 3.0 Å resolution are reported, which will contribute to future studies on ZikV infection and the development of inhibitors of ZIKV replication.
Journal ArticleDOI
Synthesis, stereochemistry and biological activity of some novel long alkyl chain substituted thiazolidin-4-ones and thiazan-4-one from 10-undecenoic acid hydrazide.
TL;DR: The synthesis of four novel compounds, including hydrazones (2), (3) and (7) exist in two conformers as synperiplanar and antiperiPlanar, and Structural assignment, stereochemistry and biological assays are discussed.
Journal ArticleDOI
Zika Virus Methyltransferase: Structure and Functions for Drug Design Perspectives.
Bruno Coutard,Karine Barral,Julie Lichière,Barbara Selisko,Baptiste Martin,Wahiba Aouadi,Miguel Ortiz Lombardia,Françoise Debart,Jean-Jacques Vasseur,Jean-Claude Guillemot,Bruno Canard,Etienne Decroly +11 more
TL;DR: It is demonstrated that the ZIKV methyltransferase methylates the mRNA cap and adenosines located in RNA sequences, and conformational specificities highlight the role of a conserved Ser/Arg motif, which participates in RNA and SAM recognition during the reaction turnover.