About: Structural Basis for Inhibiting Porcine Epidemic Diarrhea Virus Replication with the 3C-Like Protease Inhibitor GC376

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About: Structural Basis for Inhibiting Porcine Epidemic Diarrhea Virus Replication with the 3C-Like Protease Inhibitor GC376 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
has title	Structural Basis for Inhibiting Porcine Epidemic Diarrhea Virus Replication with the 3C-Like Protease Inhibitor GC376
Creator	Peng, Guiqing Shi, Yuejun Ye, Gang Tong, Xiaohan Fu, Zhen Wang, Xiaowei
topic	covid:72145127f34096ecce4d5da44c838bfffa6873c7#this
Source	Medline; PMC
abstract	Porcine epidemic diarrhea virus (PEDV), being highly virulent and contagious in piglets, has caused significant damage to the pork industries of many countries worldwide. There are no commercial drugs targeting coronaviruses (CoVs), and few studies on anti-PEDV inhibitors. The coronavirus 3C-like protease (3CL(pro)) has a conserved structure and catalytic mechanism and plays a key role during viral polyprotein processing, thus serving as an appealing antiviral drug target. Here, we report the anti-PEDV effect of the broad-spectrum inhibitor GC376 (targeting 3Cpro or 3CL(pro) of viruses in the picornavirus-like supercluster). GC376 was highly effective against the PEDV 3CL(pro) and exerted similar inhibitory effects on two PEDV strains. Furthermore, the structure of the PEDV 3CL(pro) in complex with GC376 was determined at 1.65 Å. We elucidated structural details and analyzed the differences between GC376 binding with the PEDV 3CL(pro) and GC376 binding with the transmissible gastroenteritis virus (TGEV) 3CL(pro). Finally, we explored the substrate specificity of PEDV 3CL(pro) at the P2 site and analyzed the effects of Leu group modification in GC376 on inhibiting PEDV infection. This study helps us to understand better the PEDV 3CL(pro) substrate specificity, providing information on the optimization of GC376 for development as an antiviral therapeutic against coronaviruses.
has issue date	2020-02-21(xsd:dateTime)
bibo:doi	10.3390/v12020240
bibo:pmid	32098094
has license	cc-by
sha1sum (hex)	72145127f34096ecce4d5da44c838bfffa6873c7
schema:url	https://doi.org/10.3390/v12020240
resource representing a document's title	Structural Basis for Inhibiting Porcine Epidemic Diarrhea Virus Replication with the 3C-Like Protease Inhibitor GC376
has PubMed Central identifier	PMC7077318
has PubMed identifier	32098094
schema:publication	Viruses
resource representing a document's body	covid:72145127f34096ecce4d5da44c838bfffa6873c7#body_text
is http://vocab.deri.ie/void#inDataset of	https://covidontheweb.inria.fr:4443/about/id/http/ns.inria.fr/covid19/72145127f34096ecce4d5da44c838bfffa6873c7
is schema:about of	named entity 'INHIBITORS' named entity 'LEU' named entity 'OPTIMIZATION' named entity 'EFFECTIVE' named entity 'STUDY' named entity 'PRO' named entity 'DETERMINED' named entity 'PLAYS' named entity 'ROLE' named entity 'DEVELOPMENT' named entity 'TRANSMISSIBLE GASTROENTERITIS VIRUS' named entity 'SPECTRUM' named entity 'BETTER' named entity 'SIGNIFICANT' named entity 'PROVIDING' named entity 'HIGHLY' named entity 'INHIBITING' named entity 'VIRUSES' named entity 'COMMERCIAL' named entity 'STUDIES' named entity 'inhibiting' named entity 'complex' named entity 'effects' named entity 'caused' named entity 'industries' named entity 'piglets' named entity 'targeting' named entity 'PROTEASE' named entity '1.65' named entity 'HELPS' named entity 'COUNTRIES' named entity 'COMPLEX' named entity 'BROAD' named entity 'PORK' named entity 'ANTIVIRAL DRUG' named entity 'PICORNAVIRUS' named entity 'SERVING' named entity 'GROUP' named entity 'CORONAVIRUS' named entity 'VIRULENT' named entity 'ANALYZED' named entity 'INDUSTRIES' named entity 'APPEALING' named entity 'DRUG TARGET' named entity 'DAMAGE' named entity 'BINDING' named entity 'PORCINE EPIDEMIC DIARRHEA VIRUS' named entity 'INHIBITING' named entity 'VIRUS REPLICATION' covid:arg/72145127f34096ecce4d5da44c838bfffa6873c7 named entity '3C-LIKE PROTEASE INHIBITOR' named entity 'STRUCTURAL' named entity 'BASIS' named entity 'EFFECT' named entity 'SITE' named entity 'BEING' named entity 'STRAINS' named entity 'CAUSED' named entity 'PORCINE EPIDEMIC DIARRHEA VIRUS' named entity 'INHIBITOR' named entity 'THERAPEUTIC' named entity 'SIMILAR' named entity 'ANTIVIRAL' named entity 'HERE' named entity 'DETAILS' named entity 'DRUGS TARGETING' named entity 'CATALYTIC MECHANISM' named entity 'WORLDWIDE' named entity 'STRUCTURAL' named entity 'SUBSTRATE SPECIFICITY' named entity 'STRUCTURE' named entity 'INHIBITORY' named entity 'EXERTED' named entity 'KEY'

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