skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: Gain-of-Signal Assays for Probing Inhibition of SARS-CoV-2 M[superscript pro]/3CL[superscript pro] i

Journal Article · · mBio

Research Organization:
Argonne National Laboratory (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; NCI; NIAID
OSTI ID:
1879747
Journal Information:
mBio, Vol. 13, Issue (3)
Country of Publication:
United States
Language:
ENGLISH

References (62)

Development of boceprevir: a first-in-class direct antiviral treatment for chronic hepatitis C infection: Boceprevir: a first-in-class direct antiviral journal July 2013
Taming a beast: lessons from the domestication of hepatitis C virus journal April 2019
Improving Viral Protease Inhibitors to Counter Drug Resistance journal July 2016
Coronaviruses: An Overview of Their Replication and Pathogenesis book January 2015
From SARS to MERS: crystallographic studies on coronaviral proteases enable antiviral drug design journal August 2014
Human Coronavirus: Host-Pathogen Interaction journal September 2019
Targeting SARS-CoV-2 Proteases for COVID-19 Antiviral Development journal February 2022
Design, synthesis and antiviral efficacy of a series of potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitors journal October 2008
Structure-based design, synthesis, and biological evaluation of peptidomimetic SARS-CoV 3CLpro inhibitors journal November 2007
Coronavirus Main Proteinase (3CLpro) Structure: Basis for Design of Anti-SARS Drugs journal June 2003
Production of Authentic SARS-CoV Mpro with Enhanced Activity: Application as a Novel Tag-cleavage Endopeptidase for Protein Overproduction journal February 2007
Feline coronavirus drug inhibits the main protease of SARS-CoV-2 and blocks virus replication journal August 2020
Profiling of Substrate Specificities of 3C-Like Proteases from Group 1, 2a, 2b, and 3 Coronaviruses journal November 2011
Designing a Green Fluorogenic Protease Reporter by Flipping a Beta Strand of GFP for Imaging Apoptosis in Animals journal March 2019
Development of a Fluorescence-Based, High-Throughput SARS-CoV-2 3CL pro Reporter Assay journal October 2020
Identify potent SARS-CoV-2 main protease inhibitors via accelerated free energy perturbation-based virtual screening of existing drugs journal October 2020
Discovery of SARS-CoV-2 Papain-like Protease Inhibitors through a Combination of High-Throughput Screening and a FlipGFP-Based Reporter Assay journal June 2021
Validation and invalidation of SARS-CoV-2 main protease inhibitors using the Flip-GFP and Protease-Glo luciferase assays journal April 2022
A protease-activatable luminescent biosensor and reporter cell line for authentic SARS-CoV-2 infection journal February 2022
Detecting SARS-CoV-2 3CLpro expression and activity using a polyclonal antiserum and a luciferase-based biosensor journal April 2021
Design of modular autoproteolytic gene switches responsive to anti-coronavirus drug candidates journal November 2021
Development of a Cell-Based Luciferase Complementation Assay for Identification of SARS-CoV-2 3CLpro Inhibitors journal January 2021
Sensitivity of Human Immunodeficiency Virus Type 1 to the Fusion Inhibitor T-20 Is Modulated by Coreceptor Specificity Defined by the V3 Loop of gp120 journal September 2000
A new reporter cell line to monitor HIV infection and drug susceptibility in vitro journal April 1997
Two adjacent mutations on the dimer interface of SARS coronavirus 3C-like protease cause different conformational changes in crystal structure journal June 2009
Role of proteolytic enzymes in the COVID-19 infection and promising therapeutic approaches journal December 2020
Broad-Spectrum Antivirals against 3C or 3C-Like Proteases of Picornaviruses, Noroviruses, and Coronaviruses journal August 2012
Efficacy of a 3C-like protease inhibitor in treating various forms of acquired feline infectious peritonitis journal May 2017
Discovery of (1 R ,5 S )- N -[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2( S )-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2( S )-carboxamide (SCH 503034), a Selective, Potent, Orally Bioavailable Hepatitis C Virus NS3 Protease Inhibitor:  A Potential Therapeutic Agent for the Treatment of Hepatitis C Infection journal September 2006
An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus journal October 2003
Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease journal September 2020
Malleability of the SARS-CoV-2 3CL Mpro Active-Site Cavity Facilitates Binding of Clinical Antivirals journal December 2020
Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease journal June 2020
The HIV-1 Tat Nuclear Localization Sequence Confers Novel Nuclear Import Properties journal January 1998
Design and construction of a stereochemically diverse piperazine-based DNA-encoded chemical library journal October 2021
DNA-encoded chemistry technology yields expedient access to SARS-CoV-2 M pro inhibitors journal August 2021
An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19 journal December 2021
Ethacridine inhibits SARS-CoV-2 by inactivating viral particles journal September 2021
Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors journal April 2020
Structural basis for the inhibition of SARS-CoV-2 main protease by antineoplastic drug carmofur journal May 2020
Defending Antiviral Cationic Amphiphilic Drugs That May Cause Drug-Induced Phospholipidosis journal September 2021
Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2 journal August 2021
Ebselen, Disulfiram, Carmofur, PX-12, Tideglusib, and Shikonin Are Nonspecific Promiscuous SARS-CoV-2 Main Protease Inhibitors journal October 2020
Molecular characterization of ebselen binding activity to SARS-CoV-2 main protease journal August 2020
Inhibition mechanism of SARS-CoV-2 main protease by ebselen and its derivatives journal May 2021
Hepatitis C virus protease inhibitor-resistance mutations: Our experience and review journal January 2013
Flexibility—Not just for yoga anymore! journal January 2018
The proximal proteome of 17 SARS-CoV-2 proteins links to disrupted antiviral signaling and host translation journal October 2021
N‐Terminomics for the Identification of In Vitro Substrates and Cleavage Site Specificity of the SARS‐CoV‐2 Main Protease journal November 2020
Identification of Host Cellular Protein Substrates of SARS-COV-2 Main Protease journal December 2020
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing journal April 2020
Ribozymes as Potential Anti-HIV-1 Therapeutic Agents journal March 1990
APOBEC3B is an enzymatic source of mutation in breast cancer journal February 2013
Protein production by auto-induction in high-density shaking cultures journal May 2005
Structural and Biochemical Analysis of the Dual Inhibition of MG-132 against SARS-CoV-2 Main Protease (Mpro/3CLpro) and Human Cathepsin-L journal October 2021
XDS journal January 2010
Phaser crystallographic software journal July 2007
Coot model-building tools for molecular graphics journal November 2004
Macromolecular structure determination using X-rays, neutrons and electrons: recent developments in Phenix journal October 2019
Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors journal March 2020
The preclinical inhibitor GS441524 in combination with GC376 efficaciously inhibited the proliferation of SARS-CoV-2 in the mouse respiratory tract journal January 2021
Lead compounds for the development of SARS-CoV-2 3CL protease inhibitors journal April 2021