Validation and invalidation of SARS-CoV-2 main protease inhibitors using the Flip-GFP and Protease-Glo luciferase assays

Identification of existing pharmaceuticals and herbal medicines as inhibitors of SARS-CoV-2 infection

(2021) Jia-Tsrong Jan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Bepridil is potent against SARS-CoV-2 in vitro

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Dipyridamole, chloroquine, montelukast sodium, candesartan, oxytetracycline, and atazanavir are not SARS-CoV-2 main protease inhibitors

(2021) Chunlong Ma et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

SARS-CoV-2 Mpro inhibitors with antiviral activity in a transgenic mouse model

(2021) Jingxin Qiao et al.   SCIENCE

Identification of ebselen and its analogues as potent covalent inhibitors of papain-like protease from SARS-CoV-2

(2021) Ewelina Weglarz-Tomczak et al.   Scientific Reports

The Preclinical Inhibitor GS441524 in Combination with GC376 Efficaciously Inhibited the Proliferation of SARS-CoV-2 in the Mouse Respiratory Tract

(2021) Yuejun Shi et al.   Emerging Microbes & Infections

Boceprevir, Calpain Inhibitors II and XII, and GC-376 Have Broad-Spectrum Antiviral Activity against Coronaviruses

(2021) Yanmei Hu et al.   ACS Infectious Diseases

Direct Observation of Protonation State Modulation in SARS-CoV-2 Main Protease upon Inhibitor Binding with Neutron Crystallography

(2021) Daniel W. Kneller et al.   JOURNAL OF MEDICINAL CHEMISTRY

Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors

(2021) Naoya Kitamura et al.   JOURNAL OF MEDICINAL CHEMISTRY

Efficacy of GC-376 against SARS-CoV-2 virus infection in the K18 hACE2 transgenic mouse model

(2021) C. Joaquín Cáceres et al.   Scientific Reports

Hepatitis C virus drugs that inhibit SARS-CoV-2 papain-like protease synergize with remdesivir to suppress viral replication in cell culture

(2021) Khushboo Bafna et al.   Cell Reports

Baicalein and Baicalin Inhibit SARS-CoV-2 RNA-Dependent-RNA Polymerase

(2021) Keivan Zandi et al.   Microorganisms

Ebsulfur and Ebselen as highly potent scaffolds for the development of potential SARS-CoV-2 antivirals

(2021) Le-Yun Sun et al.   BIOORGANIC CHEMISTRY

Postinfection treatment with a protease inhibitor increases survival of mice with a fatal SARS-CoV-2 infection

(2021) Chamandi S. Dampalla et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2021) Nir Drayman et al.   SCIENCE

Inhibition mechanism of SARS-CoV-2 main protease by ebselen and its derivatives

(2021) Kangsa Amporndanai et al.   Nature Communications

Ethacridine inhibits SARS-CoV-2 by inactivating viral particles

(2021) Xiaoquan Li et al.   PLoS Pathogens

Discovery of SARS-CoV-2 Papain-like Protease Inhibitors through a Combination of High-Throughput Screening and a FlipGFP-Based Reporter Assay

(2021) Chunlong Ma et al.   ACS Central Science

Recent advances in developing small-molecule inhibitors against SARS-CoV-2

(2021) Rong Xiang et al.   Acta Pharmaceutica Sinica B

Medicinal chemistry strategies towards the development of effective SARS-CoV-2 inhibitors

(2021) Shenghua Gao et al.   Acta Pharmaceutica Sinica B

An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19

(2021) Dafydd R. Owen et al.   SCIENCE

Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro

(2020) Manli Wang et al.   CELL RESEARCH

SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor

(2020) Markus Hoffmann et al.   CELL

Drug Development and Medicinal Chemistry Efforts toward SARS‐Coronavirus and Covid‐19 Therapeutics

(2020) Arun K. Ghosh et al.   ChemMedChem

Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors

(2020) Zhenming Jin et al.   NATURE

Structural basis for the inhibition of SARS-CoV-2 main protease by antineoplastic drug carmofur

(2020) Zhenming Jin et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

A Trial of Lopinavir–Ritonavir in Adults Hospitalized with Severe Covid-19

(2020) Bin Cao et al.   NEW ENGLAND JOURNAL OF MEDICINE

Antiviral Efficacies of FDA-Approved Drugs against SARS-CoV-2 Infection in Ferrets

(2020) Su-Jin Park et al.   mBio

Hydroxychloroquine, a less toxic derivative of chloroquine, is effective in inhibiting SARS-CoV-2 infection in vitro

(2020) Jia Liu et al.   Cell Discovery

Anti-SARS-CoV-2 activities in vitro of Shuanghuanglian preparations and bioactive ingredients

(2020) Hai-xia Su et al.   ACTA PHARMACOLOGICA SINICA

Atazanavir, alone or in combination with ritonavir, inhibits SARS-CoV-2 replication and pro-inflammatory cytokine production

(2020) Natalia Fintelman-Rodrigues et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro

(2020) Ka-Tim Choy et al.   ANTIVIRAL RESEARCH

Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease

(2020) Chunlong Ma et al.   CELL RESEARCH

Evaluation of SARS-CoV-2 3C-like protease inhibitors using self-assembled monolayer desorption ionization mass spectrometry

(2020) Zachary A. Gurard-Levin et al.   ANTIVIRAL RESEARCH

The SARS-CoV-2 main protease as drug target

(2020) Sven Ullrich et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of a Fluorescence-Based, High-Throughput SARS-CoV-2 3CLpro Reporter Assay

(2020) Heather M. Froggatt et al.   JOURNAL OF VIROLOGY

Lopinavir–ritonavir in patients admitted to hospital with COVID-19 (RECOVERY): a randomised, controlled, open-label, platform trial

(2020) Peter W Horby et al.   LANCET

SARS-CoV-2 Mpro inhibitors and activity-based probes for patient-sample imaging

(2020) Wioletta Rut et al.   Nature Chemical Biology

Characteristics of SARS-CoV-2 and COVID-19

(2020) Ben Hu et al.   NATURE REVIEWS MICROBIOLOGY

Identify potent SARS-CoV-2 main protease inhibitors via accelerated free energy perturbation-based virtual screening of existing drugs

(2020) Zhe Li et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Malleability of the SARS-CoV-2 3CL Mpro active site cavity facilitates binding of clinical antivirals

(2020) Daniel W. Kneller et al.   STRUCTURE

GRL-0920, an Indole Chloropyridinyl Ester, Completely Blocks SARS-CoV-2 Infection

(2020) Shin-ichiro Hattori et al.   mBio

Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2

(2020) Mohammad M. Ghahremanpour et al.   ACS Medicinal Chemistry Letters

Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease

(2020) Lifeng Fu et al.   Nature Communications

A nanoluciferase SARS-CoV-2 for rapid neutralization testing and screening of anti-infective drugs for COVID-19

(2020) Xuping Xie et al.   Nature Communications

Feline coronavirus drug inhibits the main protease of SARS-CoV-2 and blocks virus replication

(2020) Wayne Vuong et al.   Nature Communications

Crystal structure of SARS-CoV-2 papain-like protease

(2020) Xiaopan Gao et al.   Acta Pharmaceutica Sinica B

Structure-Based Virtual Screening and Biochemical Validation to Discover a Potential Inhibitor of the SARS-CoV-2 Main Protease

(2020) Akshita Gupta et al.   ACS Omega

Crystal structure of SARS-CoV-2 main protease in complex with the natural product inhibitor shikonin illuminates a unique binding mode

(2020) Jian Li et al.   Science Bulletin

Designing a Green Fluorogenic Protease Reporter by Flipping a Beta Strand of GFP for Imaging Apoptosis in Animals

(2019) Qiang Zhang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Disulfiram can inhibit MERS and SARS coronavirus papain-like proteases via different modes

(2018) Min-Han Lin et al.   ANTIVIRAL RESEARCH

Structural Basis for Inactivation ofGiardia lambliaCarbamate Kinase by Disulfiram

(2014) Andrey Galkin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Disulfiram is a direct and potent inhibitor of human O6-methylguanine-DNA methyltransferase (MGMT) in brain tumor cells and mouse brain and markedly increases the alkylating DNA damage

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