About: 6-Thioguanine blocks SARS-CoV-2 replication by inhibition of PLpro protease activities

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About: 6-Thioguanine blocks SARS-CoV-2 replication by inhibition of PLpro protease activities 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	6-Thioguanine blocks SARS-CoV-2 replication by inhibition of PLpro protease activities
Creator	Zhao, Xu Boon, Adrianus Lenschow, Deborah Perng, Yi-Chieh Affiliations, * Darling, Tamarand Huibregtse, Jon Canadeo, Larissa Harastani, Houda Swaim, Caleb
Source	BioRxiv; Medline; PMC
abstract	A recently emerged betacoronavirus, SARS-CoV-2, has led to a global health crisis that calls for the identification of effective therapeutics for COVID-19 disease. Coronavirus papain-like protease (PLpro) is an attractive drug target as it is essential for viral polyprotein cleavage and for deconjugation of ISG15, an antiviral ubiquitin-like protein. We show here that 6-Thioguanine (6-TG) inhibits SARS-CoV-2 PLpro-catalyzed viral polyprotein cleavage and ISG15 deconjugation in cells and inhibits replication of SARS-CoV-2 in Vero-E6 cells and Calu3 cells at submicromolar levels. As a well-characterized FDA-approved orally delivered drug, 6-TG represents a promising therapeutic for COVID-19 and other emerging coronaviruses. One Sentence Summary A repurposed drug that targets an essential enzymatic activity of SARS-CoV-2 represents a promising COVID-19 therapeutic.
has issue date	2020-07-02(xsd:dateTime)
bibo:doi	10.1101/2020.07.01.183020
bibo:pmid	32637945
has license	biorxiv
sha1sum (hex)	2eaf1b3d1af9a366c43f4cf84e96cefa20e2851b
schema:url	https://doi.org/10.1101/2020.07.01.183020
resource representing a document's title	6-Thioguanine blocks SARS-CoV-2 replication by inhibition of PLpro protease activities
has PubMed Central identifier	PMC7337375
has PubMed identifier	32637945
schema:publication	bioRxiv
resource representing a document's body	covid:2eaf1b3d1af9a366c43f4cf84e96cefa20e2851b#body_text
is schema:about of	named entity 'essential' named entity 'One' named entity 'drug' named entity 'therapeutic' named entity 'SARS-CoV-2' named entity 'enzymatic activity' named entity 'SARS-CoV-2' named entity 'PLpro' named entity 'conjugation' named entity 'western blotting' named entity 'Triton X-100' named entity 'IFN-γ' named entity 'Herc5' named entity 'ISG15' named entity 'ISG15' named entity 'lysis buffer' named entity 'intracellular' named entity 'antibody' named entity 'Protein A/G' named entity 'fusion protein' named entity 'lysed' named entity 'cytokine' named entity 'ISG15' named entity 'Isopropyl β-D-1-thiogalactopyranoside' named entity 'cell culture' named entity 'secretion' named entity 'clone' named entity 'co-expression' named entity 'IPTG' named entity 'Protein' named entity 'SARS-CoV-2' named entity 'IL-6' named entity 'Actin' named entity 'cytokine' named entity 'ISG15' named entity 'nsp3' named entity 'extracellular' named entity 'ISG15' named entity 'Sars-CoV-2' named entity 'IL-10' named entity 'pH 8' named entity 'cytotoxicity' named entity 'HEK293T' named entity 'Herc5' named entity 'nsp3' named entity 'dose-dependent' named entity 'ISG15' named entity 'Virus replication' named entity 'HEK293T cells' named entity 'conjugation' named entity 'E. coli' named entity 'Triton X-100' named entity 'C-terminal' named entity 'IL-6' named entity 'peer review' named entity 'ISG15' named entity 'antiviral' named entity 'PLpro' named entity 'PBS' named entity 'GSH' named entity 'extracellular' named entity 'complement' named entity 'centrifugation' named entity 'bioRxiv' named entity 'IFN-γ' named entity 'ISG15' named entity 'thiopurine' named entity 'cleavage' named entity 'cytokines' named entity 'PLpro' named entity 'serum' named entity 'viral replication'

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