ArticleACS chemical biology2021
A Clinical-Stage Cysteine Protease Inhibitor blocks SARS-CoV-2 Infection of Human and Monkey Cells.
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Article in ACS chemical biology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 71 papers.
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71citing papers in PubMed
6.8field-weighted citation impact, top 2% of its field
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Who cites it
71 citing papers in PubMed, 117 citations in OpenAlex.
- Development and preclinical evaluation of selective vinyl sulfone-based probes for PET imaging of tumor-associated cathepsins.EJNMMI radiopharmacy and chemistry · 2026Article
- Recent Advances in the Design of Inhibitors Targeting the Viral Entry and Replication of the SARS-CoV-2 Virus, Driven by In Silico Approaches.Molecules (Basel, Switzerland) · 2026Review
- Substrate Specificity and Kinetic Mechanism of the NAD+-Dependent Deacylase from Mycobacterium tuberculosis, Rv1151c (Mt-Sirt).Biochemistry · 2026Article
- Peptidomimetic α,β-Unsaturated Ethyl Esters Are Irreversible Inactivators of Human Cathepsin L and Are Potent Inhibitors of SARS-CoV-2 in Cellular Models of COVID-19.Journal of medicinal chemistry · 2026Article
- SARS-CoV-2 infection in hiPSC-derived neurons is cathepsin-dependent and causes differential accumulation of HIF1ɑ and phosphorylated tau.Molecular therapy. Nucleic acids · 2025Article
- Discovery of benzyl carbamate inhibitors of coronavirus MJournal of enzyme inhibition and medicinal chemistry · 2025Article
- Production of human cathepsins using Expi293™ mammalian cell expression system for off-target activity of cysteine protease inhibitor screening.Protein science : a publication of the Protein Society · 2025Article
- Azapeptide-Based SARS-CoV-2 Main Protease Inhibitors: Design, Synthesis, Enzyme Inhibition, Structural Determination, and Antiviral Activity.Journal of medicinal chemistry · 2025Article
- Peptidomimetic Phenoxymethyl Ketone Warheads as Potent Dual-Mode Inhibitors against SARS-CoV-2 MJournal of medicinal chemistry · 2025Article
- ACOD1-mediated lysosomal membrane permeabilization contributes toProceedings of the National Academy of Sciences of the United States of America · 2025Article
- A covalent chemical probe for Chikungunya nsP2 cysteine protease with antialphaviral activity and proteome-wide selectivity.Scientific reports · 2025Article
- Dual Inhibitors of SARS-CoV-2 3CL Protease and Human Cathepsin L Containing Glutamine Isosteres Are Anti-CoV-2 Agents.Journal of the American Chemical Society · 2025Article
- Pyrazinyl-Substituted Aminoazoles as Covalent Inhibitors of Thrombin: Synthesis, Structure, and Anticoagulant Properties.ACS pharmacology & translational science · 2025Article
- Discovery of a Potent Triazole-Based Reversible Targeted Covalent Inhibitor of Cruzipain.ACS medicinal chemistry letters · 2025Article
- Discovering novel Cathepsin L inhibitors from natural products using artificial intelligence.Computational and structural biotechnology journal · 2024Article
- Peptide Aldehydes Incorporating Thiazol-4-yl Alanine Are Potent In Vitro Inhibitors of SARS-CoV-2 Main Protease.ACS medicinal chemistry letters · 2024Article
- A Covalent Chemical Probe forResearch square · 2024Article
- Native Mass Spectrometry Reveals Binding Interactions of SARS-CoV-2 PLpro with Inhibitors and Cellular Targets.ACS infectious diseases · 2024Article
- Insights into the Main Protease of SARS-CoV-2: Thermodynamic Analysis, Structural Characterization, and the Impact of Inhibitors.Analytical chemistry · 2024Article
- Oral Pyronaridine Tetraphosphate Reduces Tissue Presence of Parasites in a Mouse Model of Chagas Disease.ACS omega · 2024Article
11 more citing papers are in PubMed but not listed here.
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Authors and funding
31 authors at 4 institutions in 2 countries.
Drake M MellottORCID 0000-0002-8043-8170
Chien-Te TsengDepartment of Microbiology and Immunology, University of Texas, Medical Branch, 3000 University Boulevard, Galveston, Texas 77755-1001, United States.
Aleksandra DrelichDepartment of Microbiology and Immunology, University of Texas, Medical Branch, 3000 University Boulevard, Galveston, Texas 77755-1001, United States.
Pavla FajtováSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.
Bala C ChennaORCID 0000-0002-2660-5302
Demetrios H Kostomiris
Jason HsuDepartment of Microbiology and Immunology, University of Texas, Medical Branch, 3000 University Boulevard, Galveston, Texas 77755-1001, United States.
Jiyun Zhu
Zane W Taylor
Klaudia I Kocurek
Vivian TatDepartment of Microbiology and Immunology, University of Texas, Medical Branch, 3000 University Boulevard, Galveston, Texas 77755-1001, United States.
Ardala Katzfuss
Linfeng LiORCID 0000-0001-6185-4999
Miriam A GiardiniSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.
Danielle SkinnerSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.
Ken HirataSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.
Michael C YoonSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.
Sungjun BeckSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.
Aaron F CarlinDepartment of Medicine, Division of Infectious Diseases and Global Public Health, University of California San Diego, La Jolla, California 92037, United States.
Alex E ClarkSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.
Laura BerettaSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.
Daniel Maneval
Vivian HookSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.ORCID 0000-0001-6461-7024
Felix Frueh
Brett L Hurst
Hong Wang
Frank M RaushelORCID 0000-0002-5918-3089
Anthony J O'DonoghueSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.ORCID 0000-0001-5695-0409
Jair Lage de Siqueira-NetoSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.
Thomas D MeekORCID 0000-0002-1931-8073
James H McKerrowSkaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.ORCID 0000-0002-5152-4627
University of California San Diego · USTexas A&M University · USThe University of Texas Medical Branch at Galveston · USUtah State University · US
Funding
World Reference Center for Emerging Viruses and Arboviruses (WRCEVA)R24AI120942 · NIAID · UNIVERSITY OF TEXAS MED BR GALVESTON · PI WEAVER, SCOTT C · 2016 to 2024
$8.5MT CELL MEMORY TO VIRUSESR01AI030048 · NIAID · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI AHMED, RAFI · 1990 to 2022
$5.2MT CELL MEMORY TO VIRUSESR37AI030048 · NIAID · EMORY UNIVERSITY · PI AHMED, RAFI · 2001 to 2010
$3.9MNIAID NIH HHS N01 AI030048NIAID NIH HHS R24 AI120942
Abstract
Host-cell cysteine proteases play an essential role in the processing of the viral spike protein of SARS coronaviruses. K777, an irreversible, covalent inactivator of cysteine proteases that has recently completed phase 1 clinical trials, reduced SARS-CoV-2 viral infectivity in several host cells: Vero E6 (EC
Indexed as
AnimalsAntiviral AgentsCathepsin LCell Line, TumorChlorocebus aethiopsCysteine Proteinase InhibitorsHumansMicrobial Sensitivity TestsPhenylalaninePiperazinesProtein DomainsProteolysisSARS-CoV-2Spike Glycoprotein, CoronavirusTosyl CompoundsVero CellsAntiviral AgentsCathepsin LCysteine Proteinase InhibitorsN-pip-phenylalanine-homophenylalanine-vinyl sulfone phenylPhenylalaninePiperazinesSpike Glycoprotein, Coronavirusspike protein, SARS-CoV-2Tosyl Compounds
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.