Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2 | Zendy

Nir Drayman | Zendy; Jennifer K. DeMarco | Zendy; Krysten A. Jones | Zendy; SaaraAnne Azizi | Zendy; Heather M. Froggatt | Zendy; Kemin Tan | Zendy; N. Maltseva | Zendy; Siquan Chen | Zendy; Vlad Nicolaescu | Zendy; Steve Dvorkin | Zendy; Kevin Furlong | Zendy; Rahul S. Kathayat | Zendy; Mason R. Firpo | Zendy; Vincent Mastrodomenico | Zendy; Emily A. Bruce | Zendy; Madaline M. Schmidt | Zendy; R. Jedrzejczak | Zendy; Miguel Ángel Muñoz-Alía | Zendy; Brooke Schuster | Zendy; Vishnu Nair | Zendy; KyuYeon Han | Zendy; Amornrat O’Brien | Zendy; Αναστασία Τοματσίδου | Zendy; Bjoern Meyer | Zendy; Marco Vignuzzi | Zendy; Dominique Missiakas | Zendy; Jason Botten | Zendy; Christopher B. Brooke | Zendy; Hyun Lee | Zendy; Susan C. Baker | Zendy; Bryan C. Mounce | Zendy; Nicholas S. Heaton | Zendy; William E. Severson | Zendy; Kenneth E. Palmer | Zendy; Bryan C. Dickinson | Zendy; A. Joachimiak | Zendy; Glenn Randall | Zendy; Savaş Tay | Zendy

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Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2

Author(s) -

Nir Drayman,

Jennifer K. DeMarco,

Krysten A. Jones,

SaaraAnne Azizi,

Heather M. Froggatt,

Kemin Tan,

N. Maltseva,

Siquan Chen,

Vlad Nicolaescu,

Steve Dvorkin,

Kevin Furlong,

Rahul S. Kathayat,

Mason R. Firpo,

Vincent Mastrodomenico,

Emily A. Bruce,

Madaline M. Schmidt,

R. Jedrzejczak,

Miguel Ángel Muñoz-Alía,

Brooke Schuster,

Vishnu Nair,

KyuYeon Han,

Amornrat O’Brien,

Αναστασία Τοματσίδου,

Bjoern Meyer,

Marco Vignuzzi,

Dominique Missiakas,

Jason Botten,

Christopher B. Brooke,

Hyun Lee,

Susan C. Baker,

Bryan C. Mounce,

Nicholas S. Heaton,

William E. Severson,

Kenneth E. Palmer,

Bryan C. Dickinson,

A. Joachimiak,

Glenn Randall,

Savaş Tay

Publication year - 2021

Publication title -

science

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 12.556

H-Index - 1186

eISSN - 1095-9203

pISSN - 0036-8075

DOI - 10.1126/science.abg5827

Subject(s) - polyproteins , coronavirus , virology , proteases , viral replication , protease , covid-19 , protease inhibitor (pharmacology) , indinavir , replication (statistics) , biology , coronaviridae , virus , medicine , enzyme , viral load , biochemistry , disease , pathology , antiretroviral therapy , infectious disease (medical specialty)

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. Draymanet 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

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