About: Inhibition of Severe Acute Respiratory Syndrome Coronavirus 2 main protease by tafenoquine in vitro

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About: Inhibition of Severe Acute Respiratory Syndrome Coronavirus 2 main protease by tafenoquine in vitro 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	Inhibition of Severe Acute Respiratory Syndrome Coronavirus 2 main protease by tafenoquine in vitro
Creator	Huang, Li-Min Chiang, Yu-Ping Tsai, Chang-Hai Chen, Jin-Shing Chen, Yeh Cho, Der-Yang Chou, Yi-Zhen Hou, Mei-Hui Huang, Bao-Yue Hung, Chian-Fang Hung, Mien-Chie Hung, Yu-Lin Jeng, Long-Bin Liu, Yi-Liang Tsai, Chia-Ling Wang, Yu-Chuan Yang, Chia-Shin Yang, Wen-Hao
Source	BioRxiv
abstract	The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) causing the current pandemic, coronavirus disease 2019 (COVID-19), has taken a huge toll on human lives and the global economy. Therefore, effective treatments against this disease are urgently needed. Here, we established a fluorescence resonance energy transfer (FRET)-based high-throughput screening platform to screen compound libraries to identify drugs targeting the SARS-CoV-2 main protease (Mpro), in particular those which are FDA-approved, to be used immediately to treat patients with COVID-19. Mpro has been shown to be one of the most important drug targets among SARS-related coronaviruses as impairment of Mpro blocks processing of viral polyproteins which halts viral replication in host cells. Our findings indicate that the anti-malarial drug tafenoquine (TFQ) induces significant conformational change in SARS-CoV-2 Mpro and diminishes its protease activity. Specifically, TFQ reduces the α-helical content of Mpro, which converts it into an inactive form. Moreover, TFQ greatly inhibits SARS-CoV-2 infection in cell culture system. Hence, the current study provides a mechanistic insight into the mode of action of TFQ against SARS-CoV-2 Mpro. Moreover, the low clinical toxicity of TFQ and its strong antiviral activity against SARS-CoV-2 should warrant further testing in clinical trials.
has issue date	2020-08-15(xsd:dateTime)
bibo:doi	10.1101/2020.08.14.250258
has license	biorxiv
sha1sum (hex)	81a21ed61594a7ae32c4f9e497ad321f32167cea
schema:url	https://doi.org/10.1101/2020.08.14.250258
resource representing a document's title	Inhibition of Severe Acute Respiratory Syndrome Coronavirus 2 main protease by tafenoquine in vitro
schema:publication	bioRxiv
resource representing a document's body	covid:81a21ed61594a7ae32c4f9e497ad321f32167cea#body_text
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