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Maltseva, Natalia Ivanovna

0000-0002-2871-465X

Mayo Clinic

Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.

Citations 1

Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2
Drayman, Nir , DeMarco, Jennifer K. , Jones, Krysten A. , Azizi, Saara‐Anne , Froggatt, Heather M. , Tan, Kemin , Maltseva, N. , Chen, Siquan, Nicolaescu, Vlad , Dvorkin, Steve, Furlong, Kevin, Firpo, Mason R. , Mastrodomenico, Vincent , Bruce, Emily A. , Schmidt, Madaline M. , Jedrzejczak, R. , Schuster, Brooke , Nair, Vishnu , Han, Kyu‐Yeon , O’Brien, Amornrat , Τοματσίδου, Αναστασία, Vignuzzi, Marco , Botten, Jason , Brooke, Christopher B. , Lee, Hyun , Severson, William E., Palmer, Kenneth E. , Dickinson, Bryan C. , Joachimiak, A. , Randall, Glenn , Tay, Savaş , Maltseva, Natalia Ivanovna , Kathayat, Rahul S , Bruce, Emily A , Schmidt, Madaline M , Jedrzejczak, Robert , Muñoz-Alía, Miguel Á , Schuster, Brooke , Nair, Vishnu , Han, Kyu-Yeon , Meyer, Bjoern , Vignuzzi, Marco , Botten, Jason W , Brooke, Christopher B , Lee, Hyun , Baker, Susan C , Mounce, Bryan C , Heaton, Nicholas S , Dickinson, Bryan C , Joachimiak, Andrzej , Randall, Glenn , Tay, Savaş , Furlong, Kevin, Muñoz-Alía, Miguel Ángel , Missiakas, Dominique M.

Science | July 20, 2021 | Volume: 373 | Issue: 6557 | Pages: 931-936

10.1126/science.abg5827 Get It

Targeting the main protease of SARS-CoV-2 Inside host cells, the RNA genome of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is translated into two polyproteins that are cleaved to give the individual viral proteins. The main viral protease, known as Mpro or 3CLpro, plays a key role in these cleavages, making it an important drug target. Drayman et al . identified eight drugs that target 3CLpro from a library of 1900 clinically safe drugs. Because of the challenge of working with SARS-CoV-2, they started by screening for drugs that inhibit the replication of a human coronavirus that causes the common cold. They then evaluated the top hits for inhibiting SARS-CoV-2 replication and for inhibiting 3CLpro. Masitinib, a broad antiviral, inhibited the main proteases of coronaviruses and picornaviruses and was effective in reducing SARS-CoV-2 replication in mice. —VV