Discovery of Di- and Trihaloacetamides as Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity

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

(2021) Jingxin Qiao et al.   SCIENCE

Challenges for Targeting SARS-CoV-2 Proteases as a Therapeutic Strategy for COVID-19

(2021) Kas Steuten et al.   ACS Infectious Diseases

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

(2021) Yanmei Hu et al.   ACS Infectious Diseases

ALG-097111, a potent and selective SARS-CoV-2 3-chymotrypsin-like cysteine protease inhibitor exhibits in vivo efficacy in a Syrian Hamster model

(2021) Koen Vandyck et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

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

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

X-ray screening identifies active site and allosteric inhibitors of SARS-CoV-2 main protease

(2021) Sebastian Günther et al.   SCIENCE

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

MPI8 is Potent against SARS‐CoV‐2 by Inhibiting Dually and Selectively the SARS‐CoV‐2 Main Protease and the Host Cathepsin L**

(2021) Xinyu R. Ma et al.   ChemMedChem

SARS-CoV-2 variants, spike mutations and immune escape

(2021) William T. Harvey et al.   NATURE REVIEWS MICROBIOLOGY

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

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

(2021) Dafydd R. Owen et al.   SCIENCE

Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19

(2021) Britton Boras et al.   Nature Communications

Learning from the Past: Possible Urgent Prevention and Treatment Options for Severe Acute Respiratory Infections Caused by 2019‐nCoV

(2020) Jared S. Morse et al.   CHEMBIOCHEM

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

Cell entry mechanisms of SARS-CoV-2

(2020) Jian Shang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease

(2020) Wenhao Dai et al.   SCIENCE

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

3C-like protease inhibitors block coronavirus replication in vitro and improve survival in MERS-CoV-infected mice

(2020) Athri D. Rathnayake et al.   Science Translational Medicine

Critical Role of Type III Interferon in Controlling SARS-CoV-2 Infection in Human Intestinal Epithelial Cells

(2020) Megan L. Stanifer et al.   Cell Reports

Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19

(2020) Robert L. Hoffman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease

(2020) Alice Douangamath 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

The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization

(2020) Atli Thorarensen et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A Quick Route to Multiple Highly Potent SARS‐CoV‐2 Main Protease Inhibitors**

(2020) Kai S. Yang et al.   ChemMedChem

Proton-Coupled Conformational Activation of SARS Coronavirus Main Proteases and Opportunity for Designing Small-Molecule Broad-Spectrum Targeted Covalent Inhibitors

(2020) Neha Verma et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Therapeutically administered ribonucleoside analogue MK-4482/EIDD-2801 blocks SARS-CoV-2 transmission in ferrets

(2020) Robert M. Cox et al.   Nature Microbiology

Can Cysteine Protease Cross-class Inhibitors Achieve Selectivity?

(2019) Lorenzo Cianni et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cysteine-reactive probes and their use in chemical proteomics

(2018) Dominic G. Hoch et al.   CHEMICAL COMMUNICATIONS

Cysteine proteases as therapeutic targets: does selectivity matter? A systematic review of calpain and cathepsin inhibitors

(2015) Marton Siklos et al.   Acta Pharmaceutica Sinica B

Discovery, Synthesis, And Structure-Based Optimization of a Series of N-(tert-Butyl)-2-(N-arylamido)-2-(pyridin-3-yl) Acetamides (ML188) as Potent Noncovalent Small Molecule Inhibitors of the Severe Acute Respiratory Syndrome Coronavirus (SARS-CoV) 3CL Protease

(2012) Jon Jacobs et al.   JOURNAL OF MEDICINAL CHEMISTRY

TMPRSS2 and TMPRSS4 Facilitate Trypsin-Independent Spread of Influenza Virus in Caco-2 Cells

(2010) S. Bertram et al.   JOURNAL OF VIROLOGY

Solid-Phase Synthesis of Azidomethylene Inhibitors Targeting Cysteine Proteases

(2008) Peng-Yu Yang et al.   ORGANIC LETTERS