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Viruses 2017, 9(9), 255;

Identification of a Novel Inhibitor against Middle East Respiratory Syndrome Coronavirus

Center for Emerging Infectious Diseases, CAS Key Laboratory of Special Pathogens and Biosafety, Wuhan Institute of Virology, Chinese Academy of Sciences, No. 44 Xiao Hong Shan, Wuhan 430071, China
University of Chinese Academy of Sciences, Beijing 100049, China
Author to whom correspondence should be addressed.
Received: 10 August 2017 / Revised: 5 September 2017 / Accepted: 6 September 2017 / Published: 14 September 2017
(This article belongs to the Section Animal Viruses)
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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. View Full-Text
Keywords: MERS-CoV; fusion inhibitor; six-helix bundle; heptad repeat; five-helix bundle MERS-CoV; fusion inhibitor; six-helix bundle; heptad repeat; five-helix bundle

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Sun, Y.; Zhang, H.; Shi, J.; Zhang, Z.; Gong, R. Identification of a Novel Inhibitor against Middle East Respiratory Syndrome Coronavirus. Viruses 2017, 9, 255.

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