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                <text>Coronavirus</text>
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                <text>Dominio científico: Coronavirus</text>
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              <text>Identification of a Novel Inhibitor against Middle East Respiratory Syndrome Coronavirus</text>
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              <text>Ya-Ping Sun, Huaidong Zhang, Jian Shi, Zhe Zhang, Rui Gong</text>
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              <text>The Middle East respiratory syndrome coronavirus (MERS-CoV) was first isolated in 2012, and circulated worldwide with high mortality. The continual outbreaks of MERS-CoV highlight the importance of developing antiviral therapeutics. Here, we rationally designed a novel fusion inhibitor named MERS-five-helix bundle (MERS-5HB) derived from the six-helix bundle (MERS-6HB) which was formed by the process of membrane fusion. MERS-5HB consists of three copies of heptad repeat 1 (HR1) and two copies of heptad repeat 2 (HR2) while MERS-6HB includes three copies each of HR1 and HR2. As it lacks one HR2, MERS-5HB was expected to interact with viral HR2 to interrupt the fusion step. What we found was that MERS-5HB could bind to HR2P, a peptide derived from HR2, with a strong affinity value (KD) of up to 0.24 nM. Subsequent assays indicated that MERS-5HB could inhibit pseudotyped MERS-CoV entry effectively with 50% inhibitory concentration (IC50) of about 1 μM. In addition, MERS-5HB significantly inhibited spike (S) glycoprotein-mediated syncytial formation in a dose-dependent manner. Further biophysical characterization showed that MERS-5HB was a thermo-stable α-helical secondary structure. The inhibitory potency of MERS-5HB may provide an attractive basis for identification of a novel inhibitor against MERS-CoV, as a potential antiviral agent.</text>
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              <text>2017</text>
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              <text>MERS-CoV, fusion inhibitor, six-helix bundle, heptad repeat, five-helix bundle</text>
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              <text>DOI: 10.3390/v9090255</text>
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          <name>Source</name>
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              <text>Viruses</text>
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          <name>Publisher</name>
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              <text>MDPI AG</text>
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          <name>Coverage</name>
          <description>The spatial or temporal topic of the resource, the spatial applicability of the resource, or the jurisdiction under which the resource is relevant</description>
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              <text>Microbiology</text>
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              <text>EN</text>
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