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Anti-Zika Activity of a Library of Synthetic Carbohydrate Receptors

机译:合成碳水化合物库文库的抗Zika活性

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摘要

Zika virus (ZIKV), a mosquito-borne flavivirus, is a global health concern because of its association with severe neurological disorders. Currently, there are no antiviral therapies that have been specifically approved to treat ZIKV, and there is an urgent need to develop effective anti-ZIKV agents. Here, we report anti-ZIKV activity of 16 synthetic carbohydrate receptors (SCRs) that inhibit ZIKV infection in Vero and HeLa cells. Using a ZIKV reporter virus particle-based infection assay, our data demonstrates these SCRs are highly potent with IC(50)s as low as 0.16 mu M and negligible toxicity at several-fold higher concentrations. Time-of-addition studies showed that these SCRs inhibit the early stages of the virus infection, which is consistent with the proposed mode of action, where the SCRs likely inhibit binding between the virus and cell-surface glycans, thereby preventing viral entry into the cells and, as such, this study demonstrates a potential new strategy against ZIKV.
机译:Zika病毒(ZIKV)是一种蚊子般的黄病毒,是全球健康问题,因为它与严重神经系统疾病的关联。 目前,没有特别批准治疗ZIKV的抗病毒疗法,迫切需要开发有效的抗ZIKV代理商。 在此,我们报告了16种合成碳水化合物受体(SCR)的抗ZIKV活性,可抑制Vero和HeLa细胞中的Zikv感染。 使用基于ZIKV报告病毒颗粒的感染测定,我们的数据表现出这些SCRS高效的IC(50)S低至0.16μm,且毒性可忽略于几倍的浓度。 添加时间的研究表明,这些SCR抑制了病毒感染的早期阶段,这与所提出的作用方式一致,其中SCR可能抑制病毒和细胞表面聚糖之间的结合,从而防止病毒进入病毒进入 细胞,因此,本研究表明了对ZIKV的潜在新策略。

著录项

  • 来源
    《Journal of Medicinal Chemistry》 |2019年第8期|共10页
  • 作者单位

    CUNY Grad Ctr Adv Sci Res Ctr Nanosci Initiat 85 St Nicholas Terrace New York NY 10031 USA;

    Texas Tech Univ Hlth Sci Ctr El Paso Dept Biomed Sci Ctr Emphasis Infect Dis 5001 El Paso Dr El Paso TX 79905 USA;

    Texas Tech Univ Hlth Sci Ctr El Paso Dept Biomed Sci Ctr Emphasis Infect Dis 5001 El Paso Dr El Paso TX 79905 USA;

    CUNY Grad Ctr Adv Sci Res Ctr Nanosci Initiat 85 St Nicholas Terrace New York NY 10031 USA;

    CUNY Grad Ctr Adv Sci Res Ctr Nanosci Initiat 85 St Nicholas Terrace New York NY 10031 USA;

    CUNY Grad Ctr Adv Sci Res Ctr Nanosci Initiat 85 St Nicholas Terrace New York NY 10031 USA;

    CUNY Grad Ctr Adv Sci Res Ctr Nanosci Initiat 85 St Nicholas Terrace New York NY 10031 USA;

    Texas Tech Univ Hlth Sci Ctr El Paso Dept Biomed Sci Ctr Emphasis Infect Dis 5001 El Paso Dr El Paso TX 79905 USA;

    CUNY Grad Ctr Adv Sci Res Ctr Nanosci Initiat 85 St Nicholas Terrace New York NY 10031 USA;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
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