ArticleACS pharmacology & translational science2020
Targeting ACE2-RBD Interaction as a Platform for COVID-19 Therapeutics: Development and Drug-Repurposing Screen of an AlphaLISA Proximity Assay.
Article in ACS pharmacology & translational science, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
43 citing papers in PubMed.
- Discovery of SARS-CoV-2 Nsp14-Methyltransferase (MTase) Inhibitors by Harnessing Scaffold-Centric Exploration of the Ultra Large Chemical Space.ACS pharmacology & translational science · 2025Article
- Rapid luminescence-based screening method for SARS- CoV-2 inhibitors discovery.SLAS discovery : advancing life sciences R & D · 2025Article
- Binding Activity Classification of Anti-SARS-CoV-2 Molecules using Deep Learning Across Multiple AssaysBalkan medical journal · 2024Article
- Significance of nitrosative stress and glycoxidation products in the diagnosis of COVID-19.Scientific reports · 2024Article
- Redox Biomarkers - An Effective Tool for Diagnosing COVID-19 Patients and Convalescents.Journal of inflammation research · 2024Article
- Main and papain-like proteases as prospective targets for pharmacological treatment of coronavirus SARS-CoV-2.RSC advances · 2023Review
- Screening Drugs for Broad-Spectrum, Host-Directed Antiviral Activity: Lessons from the Development of Probenecid for COVID-19.Viruses · 2023Article
- High-Throughput Assay for Identifying Diverse Antagonists of the Binding Interaction between the ACE2 Receptor and the Dynamic Spike Proteins of SARS-CoV-2.ACS infectious diseases · 2022Article
- Celastrol: A lead compound that inhibits SARS-CoV-2 replication, the activity of viral and human cysteine proteases, and virus-induced IL-6 secretion.Drug development research · 2022Article
- Novel Regioselective Approach to Cyclize Phage-Displayed Peptides in Combination with Epitope-Directed Selection to Identify a Potent Neutralizing Macrocyclic Peptide for SARS-CoV-2.ACS chemical biology · 2022Article
- Structural genetics of circulating variants affecting the SARS-CoV-2 spike/human ACE2 complex.Journal of biomolecular structure & dynamics · 2022Article
- Genetically Engineered MRI-Trackable Extracellular Vesicles as SARS-CoV-2 Mimetics for Mapping ACE2 BindingACS nano · 2022Article
- Allosteric Binders of ACE2 Are Promising Anti-SARS-CoV-2 Agents.ACS pharmacology & translational science · 2022Article
- Allosteric binders of ACE2 are promising anti-SARS-CoV-2 agents.bioRxiv : the preprint server for biology · 2022Article
- SARS-COV-2 spike binding to ACE2 in living cells monitored by TR-FRET.Cell chemical biology · 2022Article
- SARS-CoV-2 Nucleocapsid Protein TR-FRET Assay Amenable to High Throughput Screening.ACS pharmacology & translational science · 2022Article
- A humanized nanobody phage display library yields potent binders of SARS CoV-2 spike.PloS one · 2022Article
- Small-molecule compound from AlphaScreen disrupts tau-glycan interface.Frontiers in molecular biosciences · 2022Article
- Screening S protein - ACE2 blockers from natural products: Strategies and advances in the discovery of potential inhibitors of COVID-19.European journal of medicinal chemistry · 2021Review
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The COVID-19 pandemic, caused by SARS-CoV-2, is a pressing public health emergency garnering a rapid response from scientists across the globe. Host cell invasion is initiated through direct binding of the viral spike protein to the host receptor angiotensin-converting enzyme 2 (ACE2). Disrupting the spike protein-ACE2 interaction is a potential therapeutic target for treating COVID-19. We have developed a proximity-based AlphaLISA assay to measure the binding of SARS-CoV-2 spike protein receptor binding domain (RBD) to ACE2. Utilizing this assay platform, a drug-repurposing screen against 3384 small-molecule drugs and preclinical compounds was carried out, yielding 25 high-quality primary hits, of which only corilagin was validated in cherry-picking. This established AlphaLISA RBD-ACE2 platform can facilitate evaluation of biologics or small molecules that can perturb this essential viral-host interaction to further the development of interventions to address the global health pandemic.
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Registered trials
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.