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  • Malleability of the SARS-CoV-2 3CL M(pro) Active-Site Cavity Facilitates Binding of Clinical Antivirals #MMPMID33152262
  • Kneller DW; Galanie S; Phillips G; O'Neill HM; Coates L; Kovalevsky A
  • Structure 2020[Dec]; 28 (12): 1313-1320.e3 PMID33152262show ga
  • The COVID-19 pandemic caused by SARS-CoV-2 requires rapid development of specific therapeutics and vaccines. The main protease of SARS-CoV-2, 3CL M(pro), is an established drug target for the design of inhibitors to stop the virus replication. Repurposing existing clinical drugs can offer a faster route to treatments. Here, we report on the binding mode and inhibition properties of several inhibitors using room temperature X-ray crystallography and in vitro enzyme kinetics. The enzyme active-site cavity reveals a high degree of malleability, allowing aldehyde leupeptin and hepatitis C clinical protease inhibitors (telaprevir, narlaprevir, and boceprevir) to bind and inhibit SARS-CoV-2 3CL M(pro). Narlaprevir, boceprevir, and telaprevir are low-micromolar inhibitors, whereas the binding affinity of leupeptin is substantially weaker. Repurposing hepatitis C clinical drugs as COVID-19 treatments may be a useful option to pursue. The observed malleability of the enzyme active-site cavity should be considered for the successful design of specific protease inhibitors.
  • |*Antiviral Agents/pharmacology[MESH]
  • |*Betacoronavirus/metabolism[MESH]
  • |*COVID-19[MESH]
  • |*Coronavirus Infections/drug therapy[MESH]
  • |Catalytic Domain[MESH]
  • |Crystallography, X-Ray[MESH]
  • |Cysteine Endopeptidases/metabolism[MESH]
  • |Humans[MESH]
  • |Pandemics[MESH]
  • |Protease Inhibitors/pharmacology[MESH]
  • |SARS-CoV-2[MESH]
  • |Temperature[MESH]
  • |Viral Nonstructural Proteins[MESH]

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  • suck abstract from ncbi

    1313 12.28 2020