About: Substrate specificity profiling of SARS-CoV-2 main protease enables design of activity-based probes for patient-sample imaging

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About: Substrate specificity profiling of SARS-CoV-2 main protease enables design of activity-based probes for patient-sample imaging Goto Sponge NotDistinct Permalink

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

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Substrate specificity profiling of SARS-CoV-2 main protease enables design of activity-based probes for patient-sample imaging
Creator	Hilgenfeld, Rolf Drag, Marcin Rut, Wioletta Sun, Xinyuanyuan Zhang, Linlin Groborz, Katarzyna Zmudzinski, Mikolaj
Source	BioRxiv; MedRxiv
abstract	In December 2019, the first cases of infection with a novel coronavirus, SARS-CoV-2, were diagnosed in Wuhan, China. Due to international travel and human-to-human transmission, the virus spread rapidly inside and outside of China. Currently, there is no effective antiviral treatment for coronavirus disease 2019 (COVID-19); therefore, research efforts are focused on the rapid development of vaccines and antiviral drugs. The SARS-CoV-2 main protease constitutes one of the most attractive antiviral drug targets. To address this emerging problem, we have synthesized a combinatorial library of fluorogenic substrates with glutamine in the P1 position. We used it to determine the substrate preferences of the SARS-CoV and SARS-CoV-2 main proteases, using natural and a large panel of unnatural amino acids. On the basis of these findings, we designed and synthesized an inhibitor and two activity-based probes, for one of which we determined the crystal structure of its complex with the SARS-CoV-2 Mpro. Using this approach we visualized SARS-CoV-2 active Mpro within nasopharyngeal epithelial cells of a patient with active COVID-19 infection. The results of our work provide a structural framework for the design of inhibitors as antiviral agents or diagnostic tests.
has issue date	2020-06-08(xsd:dateTime)
bibo:doi	10.1101/2020.03.07.981928
has license	biorxiv
sha1sum (hex)	3ebbcdddb122f405061bb5e1ddcf94abe9258d58
schema:url	https://doi.org/10.1101/2020.03.07.981928
resource representing a document's title	Substrate specificity profiling of SARS-CoV-2 main protease enables design of activity-based probes for patient-sample imaging
schema:publication	bioRxiv
resource representing a document's body	covid:3ebbcdddb122f405061bb5e1ddcf94abe9258d58#body_text
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