About: Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors

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About: Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors Goto Sponge NotDistinct Permalink

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

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors
Creator	Jiang, Shibo Wang, Chao Xia, Shuai Zhang, Peiyu Liu, Keliang Zhang, Tianhong Meng, Guangpeng Wang, Weicong Tian, Yangli
Source	Medline; PMC
abstract	[Image: see text] The hexameric α-helical coiled-coil formed between the C-terminal and N-terminal heptad repeat (CHR and NHR) regions of class I viral fusion proteins plays an important role in mediating the fusion of the viral and cellular membranes and provides a clear starting point for molecular mimicry that drives viral fusion inhibitor design. Unfortunately, such peptide mimicry of the short α-helical region in the CHR of Middle East respiratory syndrome coronavirus (MERS-CoV) spike protein has been thwarted by the loss of the peptide’s native α-helical conformation when taken out of the parent protein structure. Here, we describe that appropriate all-hydrocarbon stapling of the short helical portion-based peptide to reinforce its bioactive secondary structure remarkably improves antiviral potency. The resultant stapled peptide P21S10 could effectively inhibit infection by MERS-CoV pseudovirus and its spike protein-mediated cell–cell fusion; additionally, P21S10 exhibits improved pharmacokinetic properties than HR2P-M2, suggesting strong potential for development as an anti-MERS-CoV therapeutic.
has issue date	2018-02-14(xsd:dateTime)
bibo:doi	10.1021/acs.jmedchem.7b01732
bibo:pmid	29442512
has license	bronze-oa
sha1sum (hex)	47210283bc9769643f8026b4df63295b65e782e5
schema:url	https://doi.org/10.1021/acs.jmedchem.7b01732
resource representing a document's title	Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors
has PubMed Central identifier	PMC7075646
has PubMed identifier	29442512
schema:publication	Journal of Medicinal Chemistry
resource representing a document's body	covid:47210283bc9769643f8026b4df63295b65e782e5#body_text
is schema:about of	named entity 'class I' named entity 'α-helical' named entity 'potency' named entity 'improved' named entity 'α-helical' named entity 'coiled-coil' named entity 'protein structure' named entity 'REPEAT' named entity 'VIRAL FUSION PROTEINS' named entity 'PARENT' named entity 'CELL' named entity 'CHR' named entity 'STAPLING' named entity 'POTENCY' named entity 'COILED-COIL' named entity 'MEDIATING' named entity 'HELICAL' named entity 'THERAPEUTIC' named entity 'PSEUDOVIRUS' named entity 'CLASS I' named entity 'TAKEN OUT' named entity '27S' named entity 'STRONG' named entity 'MIMICRY' named entity 'POTENTIAL' named entity 'PLAYS' named entity 'ROLE' named entity 'SPIKE PROTEIN' named entity 'VIRAL' named entity 'DEVELOPMENT' named entity 'HYDROCARBON' named entity 'STARTING POINT' named entity 'DESCRIBE' named entity 'CLEAR' covid:arg/47210283bc9769643f8026b4df63295b65e782e5 named entity 'NATIVE' named entity 'PROTEIN STRUCTURE' named entity 'ITS' named entity 'APPROPRIATE' named entity 'IMPROVED' named entity 'BASED' named entity 'REGIONS' named entity 'CONFORMATION' named entity 'PORTION' named entity 'DESIGN' named entity 'N-TERMINAL ' named entity 'PROVIDES' named entity 'ANTIVIRAL' named entity 'INFECTION' named entity 'HERE' named entity 'FORMED' named entity 'REGION' named entity 'IMPORTANT' named entity 'CELLULAR' named entity 'PROPERTIES' named entity 'FUSION INHIBITORS' named entity 'DRIVES' named entity 'PROTEIN ' named entity 'EXHIBITS' named entity 'SHORT' named entity 'VIRAL AND' named entity 'FUSION INHIBITOR' named entity 'LOSS OF' named entity 'MIDDLE EAST RESPIRATORY SYNDROME CORONAVIRUS' named entity 'IMPROVES' named entity 'MEDIATED' named entity 'C-TERMINAL' named entity 'FUSION' named entity 'MEMBRANES' named entity 'SECONDARY STRUCTURE' named entity 'PHARMACOKINETIC' named entity 'PEPTIDE' named entity 'MOLECULAR MIMICRY'

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