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Structural plasticity of SARS-CoV-2 3CL Mpro active site cavity revealed by room temperature X-ray crystallography

Daniel W. Kneller, G.N. Phillips, Hugh O’Neill, R. Jedrzejczak, Lucy Stols, Paul Langan, A. Joachimiak, Leighton Coates, Andrey Kovalevsky

2020Nature Communications498 citationsDOIOpen Access PDF

Abstract

Abstract The COVID-19 disease caused by the SARS-CoV-2 coronavirus has become a pandemic health crisis. An attractive target for antiviral inhibitors is the main protease 3CL M pro due to its essential role in processing the polyproteins translated from viral RNA. Here we report the room temperature X-ray structure of unliganded SARS-CoV-2 3CL M pro , revealing the ligand-free structure of the active site and the conformation of the catalytic site cavity at near-physiological temperature. Comparison with previously reported low-temperature ligand-free and inhibitor-bound structures suggest that the room temperature structure may provide more relevant information at physiological temperatures for aiding in molecular docking studies.

Topics & Concepts

PolyproteinsActive siteCoronavirus disease 2019 (COVID-19)Docking (animal)Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)Ligand (biochemistry)CoronavirusCrystallographyChemistryBinding siteRNAProtein structure2019-20 coronavirus outbreakProteaseComputational biologyBiophysicsVirologyBiologyCatalysisMedicineEnzymeBiochemistryInfectious disease (medical specialty)GeneNursingOutbreakDiseasePathologyReceptorSARS-CoV-2 and COVID-19 ResearchComputational Drug Discovery MethodsRNA and protein synthesis mechanisms
Structural plasticity of SARS-CoV-2 3CL Mpro active site cavity revealed by room temperature X-ray crystallography | Litcius