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A Fluorogenic Peptide Cleavage Assay to Screen for Proteolytic Activity: Applications for coronavirus spike protein activation
Published on: January 9, 2019
Lead compounds for the development of SARS-CoV-2 3CL protease inhibitors
Sho Iketani1,2, Farhad Forouhar3, Hengrui Liu4
1Aaron Diamond AIDS Research Center, Columbia University Irving Medical Center, New York, NY, USA.
Abstract:
We report the identification of three structurally diverse compounds - compound 4, GC376, and MAC-5576 - as inhibitors of the SARS-CoV-2 3CL protease. Structures of each of these compounds in complex with the protease revealed strategies for further development, as well as general principles for designing SARS-CoV-2 3CL protease inhibitors. These compounds may therefore serve as leads for the basis of building effective SARS-CoV-2 3CL protease inhibitors.
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