An Overview of Severe Acute Respiratory Syndrome–Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy

By Thanigaimalai Pillaiyar, M. Manickam, V. Namasivayam, Y. Hayashi, Sang-hun Jung. Journal of Medicinal Chemistry, 2016

676 citations recorded by the source corpus.

Severe acute respiratory syndrome (SARS) is caused by a newly emerged coronavirus that infected more than 8000 individuals and resulted in more than 800 (10–15%) fatalities in 2003. The causative agent of SARS has been identified as a novel human coronavirus (SARS-CoV), and its viral protease, SARS-CoV 3CLpro, has been shown to be essential for replication and has hence been recognized as a potent drug target for SARS infection. Currently, there is no effective treatment for this epidemic despite the intensive research that has been undertaken since 2003 (over 3500 publications). This perspective focuses on the status of various efficacious anti-SARS-CoV 3CLpro chemotherapies discovered during the last 12 years (2003–2015) from all sources, including laboratory synthetic methods, natural products, and virtual screening. We describe here mainly peptidomimetic and small molecule inhibitors of SARS-CoV 3CLpro. Attempts have been made to provide a complete description of the structural features and binding modes of these inhibitors under many conditions.

Subfields: Computational Theory and Mathematics, Infectious Diseases, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/d2934299701c3e2126efae7a82a75a6e8038af50

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Citations in the corpus

Novel 2019 coronavirus structure, mechanism of action, antiviral drug promises and rule out against its treatment (2020, background): “approach toward COVID-19 treatment (Anand et al., 2003; Pillaiyar et al., 2016; Yang et al., 2003).”
The SARS-CoV-2 main protease as drug target (2020, neutral): “Several flavonoids and derivatives had previously been reported to inhibit the activity of SARSCoV M.(72,100) A fragment screening has produced several crystal structures of fragments bound to SARS-CoV-2 M, including covalent modifiers of Cys145.”