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From the Wuhan-Hu-1 strain to the XD and XE variants: is targeting the SARS-CoV-2 spike protein still a pharmaceutically relevant option against COVID-19?
Pavan, Matteo; Bassani, Davide; Sturlese, Mattia; Moro, Stefano.
  • Pavan M; Molecular Modeling Section (MMS), Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Padova, Italy.
  • Bassani D; Molecular Modeling Section (MMS), Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Padova, Italy.
  • Sturlese M; Molecular Modeling Section (MMS), Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Padova, Italy.
  • Moro S; Molecular Modeling Section (MMS), Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Padova, Italy.
J Enzyme Inhib Med Chem ; 37(1): 1704-1714, 2022 Dec.
Article in English | MEDLINE | ID: covidwho-1886330
ABSTRACT
Since the outbreak of the COVID-19 pandemic in December 2019, the SARS-CoV-2 genome has undergone several mutations. The emergence of such variants has resulted in multiple pandemic waves, contributing to sustaining to date the number of infections, hospitalisations, and deaths despite the swift development of vaccines, since most of these mutations are concentrated on the Spike protein, a viral surface glycoprotein that is the main target for most vaccines. A milestone in the fight against the COVID-19 pandemic has been represented by the development of Paxlovid, the first orally available drug against COVID-19, which acts on the Main Protease (Mpro). In this article, we analyse the structural features of both the Spike protein and the Mpro of the recently reported SARS-CoV-2 variant XE, as well the closely related XD and XF ones, discussing their impact on the efficacy of existing treatments against COVID-19 and on the development of future ones.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Spike Glycoprotein, Coronavirus / COVID-19 Drug Treatment Topics: Vaccines / Variants Limits: Humans Language: English Journal: J Enzyme Inhib Med Chem Journal subject: Biochemistry / Chemistry Year: 2022 Document Type: Article Affiliation country: 14756366.2022.2081847

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Spike Glycoprotein, Coronavirus / COVID-19 Drug Treatment Topics: Vaccines / Variants Limits: Humans Language: English Journal: J Enzyme Inhib Med Chem Journal subject: Biochemistry / Chemistry Year: 2022 Document Type: Article Affiliation country: 14756366.2022.2081847