Skip to main content
OSTI.GOVU.S. Department of Energy Office of Scientific and Technical Information
U.S. Department of Energy
Office of Scientific and Technical Information
 

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

Journal Article · · Science
; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; more »; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; « less

Research Organization:
Argonne National Laboratory (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; FOREIGN
OSTI ID:
1844723
Journal Information:
Science, Vol. 374
Country of Publication:
United States
Language:
ENGLISH

References (53)

Repurposed Antiviral Drugs for Covid-19 — Interim WHO Solidarity Trial Results February 2021
Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing July 2020
SARS-CoV-2 infection is effectively treated and prevented by EIDD-2801 February 2021
AT-527, a Double Prodrug of a Guanosine Nucleotide Analog, Is a Potent Inhibitor of SARS-CoV-2 In Vitro and a Promising Oral Antiviral for Treatment of COVID-19 March 2021
A new coronavirus associated with human respiratory disease in China February 2020
A pneumonia outbreak associated with a new coronavirus of probable bat origin February 2020
An Overview of Severe Acute Respiratory Syndrome–Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy February 2016
Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors April 2020
On the size of the active site in proteases. I. Papain April 1967
SARS-CoV-2 Mpro inhibitors and activity-based probes for patient-sample imaging October 2020
Coronavirus Main Proteinase (3CLpro) Structure: Basis for Design of Anti-SARS Drugs June 2003
α-Ketoamides as Broad-Spectrum Inhibitors of Coronavirus and Enterovirus Replication: Structure-Based Design, Synthesis, and Activity Assessment February 2020
Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS January 2016
A Journey around the Medicinal Chemistry of Hepatitis C Virus Inhibitors Targeting NS4B: From Target to Preclinical Drug Candidates August 2015
SARS-CoV-2 M pro inhibitors with antiviral activity in a transgenic mouse model February 2021
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19 October 2020
Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors March 2020
A Comparative Analysis of SARS-CoV-2 Antivirals Characterizes 3CL pro Inhibitor PF-00835231 as a Potential New Treatment for COVID-19 April 2021
Development of a new permeability assay using low‐efflux MDCKII cells November 2011
Molecular Properties That Influence the Oral Bioavailability of Drug Candidates June 2002
Reversible covalent inhibition of papain by a peptide nitrile. Carbon-13 NMR evidence for a thioimidate ester adduct March 1986
Design, synthesis and crystallographic analysis of nitrile-based broad-spectrum peptidomimetic inhibitors for coronavirus 3C-like proteases January 2013
Design and synthesis of new tripeptide-type SARS-CoV 3CL protease inhibitors containing an electrophilic arylketone moiety January 2013
Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors January 2000
The Intestinal First-pass Metabolism of Substrates of CYP3A4 and P-glycoprotei—Quantitative Analysis Based on Information from the Literature January 2003
Validated Assays for Human Cytochrome p450 Activities May 2004
A small molecule compound with an indole moiety inhibits the main protease of SARS-CoV-2 and blocks virus replication January 2021
Origin and evolution of pathogenic coronaviruses December 2018
Organic Cation Transporters (OCTs) in EpiAirway™, a Cellular Model of Normal Human Bronchial Epithelium May 2020
Pharmacokinetic/Pharmacodynamic Predictors of Clinical Potency for Hepatitis C Virus Nonnucleoside Polymerase and Protease Inhibitors April 2012
A Mouse-Adapted SARS-CoV-2 Induces Acute Lung Injury and Mortality in Standard Laboratory Mice November 2020
Development and validation of a 96-well equilibrium dialysis apparatus for measuring plasma protein binding May 2003
Darunavir: A Review of its Use in the Management of HIV Infection in Adults January 2009
Lopinavir/Ritonavir: A Review of its Use in the Management of HIV Infection January 2003
Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors December 2013
Development of potent dipeptide-type SARS-CoV 3CL protease inhibitors with novel P3 scaffolds: Design, synthesis, biological evaluation, and docking studies October 2013
Data processing and analysis with the autoPROC toolbox March 2011
Phaser crystallographic software July 2007
Molecular replacement with MOLREP December 2009
Overview of the CCP 4 suite and current developments March 2011
Features and development of Coot March 2010
On the use of the merging R factor as a quality indicator for X-ray data April 1997
Linking Crystallographic Model and Data Quality May 2012
Evaluating the 3C-like protease activity of SARS-Coronavirus: Recommendations for standardized assays for drug discovery April 2008
Broad-Spectrum Antivirals against 3C or 3C-Like Proteases of Picornaviruses, Noroviruses, and Coronaviruses August 2012
A Simple Method of Estimating Fifty per cent Endpoints12 May 1938
Evaluation of the rodent micronucleus assay by a 28-day treatment protocol: Summary of the 13th Collaborative Study by the Collaborative Study Group for the Micronucleus Test (CSGMT)/Environmental Mutagen Society of Japan (JEMS)-Mammalian Mutagenicity Study Group (MMS) January 2001
In vivo rodent erythrocyte micronucleus assay. II. Some aspects of protocol design including repeated treatments, integration with toxicity testing, and automated scoring January 2000
Mutagen testing using TRP+ reversion in Escherichia coli February 1976
Revised methods for the Salmonella mutagenicity test March 1983
Report from the In Vitro Micronucleus Assay Working Group January 2000
The detection and assessment of the aneugenic potential environmental chemicals: the European Community Aneuploidy Project May 1993
Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction December 1973

Similar Records

Related Subjects