About: Peptide-Based Membrane Fusion Inhibitors Targeting HCoV-229E Spike Protein HR1 and HR2 Domains

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About: Peptide-Based Membrane Fusion Inhibitors Targeting HCoV-229E Spike Protein HR1 and HR2 Domains 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
title	Peptide-Based Membrane Fusion Inhibitors Targeting HCoV-229E Spike Protein HR1 and HR2 Domains
Creator	Jiang, Shibo Lu, Lu Xia, Shuai Xu, Wei Wang, Qian »more»
source	Medline; PMC
abstract	Human coronavirus 229E (HCoV-229E) infection in infants, elderly people, and immunocompromised patients can cause severe disease, thus calling for the development of effective and safe therapeutics to treat it. Here we reported the design, synthesis and characterization of two peptide-based membrane fusion inhibitors targeting HCoV-229E spike protein heptad repeat 1 (HR1) and heptad repeat 2 (HR2) domains, 229E-HR1P and 229E-HR2P, respectively. We found that 229E-HR1P and 229E-HR2P could interact to form a stable six-helix bundle and inhibit HCoV-229E spike protein-mediated cell-cell fusion with IC(50) of 5.7 and 0.3 µM, respectively. 229E-HR2P effectively inhibited pseudotyped and live HCoV-229E infection with IC(50) of 0.5 and 1.7 µM, respectively. In a mouse model, 229E-HR2P administered intranasally could widely distribute in the upper and lower respiratory tracts and maintain its fusion-inhibitory activity. Therefore, 229E-HR2P is a promising candidate for further development as an antiviral agent for the treatment and prevention of HCoV-229E infection.
has issue date	2018-02-06(xsd:dateTime)
bibo:doi	10.3390/ijms19020487
bibo:pmid	29415501
has license	cc-by
sha1sum (hex)	e5ee01ea0acff01da191ffff2d9fbef2f9aebff7
schema:url	https://doi.org/10.3390/ijms19020487
resource representing a document's title	Peptide-Based Membrane Fusion Inhibitors Targeting HCoV-229E Spike Protein HR1 and HR2 Domains
has PubMed Central identifier	PMC5855709
has PubMed identifier	29415501
schema:publication	Int J Mol Sci
resource representing a document's body	covid:e5ee01ea0acff01da191ffff2d9fbef2f9aebff7#body_text
is schema:about of	named entity 'effectively' named entity 'HR2' named entity 'model' named entity 'antiviral agent' named entity 'fusion' »more»

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