About: Identification of a Novel Inhibitor against Middle East Respiratory Syndrome Coronavirus

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About: Identification of a Novel Inhibitor against Middle East Respiratory Syndrome Coronavirus Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Identification of a Novel Inhibitor against Middle East Respiratory Syndrome Coronavirus
Creator	Gong, Rui Shi, Jian Sun, Yaping Zhang, Huaidong Zhang, Zhe
source	Medline; PMC
abstract	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 (K(D)) of up to 0.24 nM. Subsequent assays indicated that MERS-5HB could inhibit pseudotyped MERS-CoV entry effectively with 50% inhibitory concentration (IC(50)) 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.
has issue date	2017-09-14(xsd:dateTime)
bibo:doi	10.3390/v9090255
bibo:pmid	28906430
has license	cc-by
sha1sum (hex)	dc180c51f54487e4bbbd129c1cc2e30deacd3181
schema:url	https://doi.org/10.3390/v9090255
resource representing a document's title	Identification of a Novel Inhibitor against Middle East Respiratory Syndrome Coronavirus
has PubMed Central identifier	PMC5618021
has PubMed identifier	28906430
schema:publication	Viruses
resource representing a document's body	covid:dc180c51f54487e4bbbd129c1cc2e30deacd3181#body_text
is schema:about of	covid:arg/dc180c51f54487e4bbbd129c1cc2e30deacd3181 named entity 'MERS-CoV' named entity 'HR2' named entity 'antiviral' named entity 'MERS-CoV' named entity 'membrane fusion' named entity 'Middle East respiratory syndrome coronavirus' named entity 'fusion inhibitor' named entity 'heptad repeat' named entity 'pseudotyped' named entity 'peptide' named entity 'dissociation constant' named entity 'cell fusion' named entity 'MERS-CoV' named entity 'PBS' named entity 'MERS-CoV' named entity 'severe acute respiratory syndrome coronavirus' named entity 'heptad repeat' named entity 'protein' named entity 'EGFP' named entity 'EGFP' named entity 'binding affinity' named entity 'MERS-CoV' named entity 'MERS-CoV' named entity 'MERS-CoV' named entity 'Qiagen' named entity 'MERS-CoV' named entity 'fusion core' named entity 'Absorbance' named entity '293T cells' named entity 'IC50' named entity 'MERS-CoV' named entity 'HR2' named entity 'gene' named entity 'protein' named entity '293T cells' named entity 'protein' named entity 'HR2' named entity 'ultraviolet' named entity '293T cells' named entity 'pseudovirus' named entity 'protein' named entity 'Germany' named entity 'MERS-CoV' named entity 'dipeptidyl peptidase-4' named entity 'fusion core' named entity '32 nM' named entity 'fusion core' named entity 'Bovine serum albumin' named entity 'virus entry' named entity 'Protein' named entity 'Huh-7' named entity '293T' named entity 'vesicular stomatitis virus' named entity 'vector' named entity 'pseudovirus' named entity 'fusion core' named entity 'MERS-CoV' named entity 'cell fusion' named entity 'plasmid' named entity 'cytotoxicity' named entity 'RBD' named entity 'VSV' named entity 'CCK-8' named entity 'renal failure' named entity 'GE Healthcare' named entity 'HR2' named entity 'amino acid' named entity 'Escherichia coli' named entity 'gp41' named entity 'SEC' named entity 'China' named entity 'HR1' named entity 'Huh-7' named entity 'MERS-CoV' named entity 'protein' named entity 'Peroxidase'

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