Link to bioRxiv paper:

http://biorxiv.org/cgi/content/short/2020.08.03.234872v1?rss=1

Authors: Kreutzer, A. G., Krumberger, M., Parrocha, C. M. T., Morris, M. A., Guaglianone, G., Nowick, J. S.

Abstract:

This paper presents the design and study of a first-in-class cyclic peptide inhibitor against the SARS-CoV-2 main protease (Mpro). The cyclic peptide inhibitor is designed to mimic the conformation of a substrate at a C-terminal autolytic cleavage site of Mpro. Synthesis and evaluation of a first-generation cyclic peptide inhibitor reveals that the inhibitor is active against Mpro in vitro and is non-toxic toward human cells in culture. The initial hit described in this manuscript, UCI-1, lays the groundwork for the development of additional cyclic peptide inhibitors against Mpro with improved activities.

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