About: Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors

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About: Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors Goto Sponge NotDistinct Permalink

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

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors
Creator	Liang, Po-Huang Kim, Chonsaeng Shie, Jiun-Jie Kim, Meehyein Kumar, Vathan Bon Ku, Keun Go, Yun Huang, Kai-Fa Shin, Jin
source	Elsevier; Medline; PMC
abstract	Abstract Middle East respiratory syndrome coronavirus (MERS-CoV) causes severe acute respiratory illness with fever, cough and shortness of breath. Up to date, it has resulted in 1826 human infections, including 649 deaths. Analogous to picornavirus 3C protease (3Cpro), 3C-like protease (3CLpro) is critical for initiation of the MERS-CoV replication cycle and is thus regarded as a validated drug target. As presented here, our peptidomimetic inhibitors of enterovirus 3Cpro (6b, 6c and 6d) inhibited 3CLpro of MERS-CoV and severe acute respiratory syndrome coronavirus (SARS-CoV) with IC50 values ranging from 1.7 to 4.7 μM and from 0.2 to 0.7 μM, respectively. In MERS-CoV-infected cells, the inhibitors showed antiviral activity with EC50 values ranging from 0.6 to 1.4 μM, by downregulating the viral protein production in cells as well as reducing secretion of infectious viral particles into culture supernatants. They also suppressed other α- and β-CoVs from human and feline origin. These compounds exhibited good selectivity index (over 70 against MERS-CoV) and could lead to the development of broad-spectrum antiviral drugs against emerging CoVs and picornaviruses.
has issue date	2017-05-31(xsd:dateTime)
bibo:doi	10.1016/j.antiviral.2017.02.007
bibo:pmid	28216367
has license	els-covid
sha1sum (hex)	aa3bf55b8d7c751c5dc8d18c208e8e1fd9064664
schema:url	https://doi.org/10.1016/j.antiviral.2017.02.007
resource representing a document's title	Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors
has PubMed Central identifier	PMC7113684
has PubMed identifier	28216367
schema:publication	Antiviral Research
resource representing a document's body	covid:aa3bf55b8d7c751c5dc8d18c208e8e1fd9064664#body_text
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