ArticleAntimicrobial agents and chemotherapy2016
Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 Replication.
Article in Antimicrobial agents and chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 57 papers.
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Who cites it
57 citing papers in PubMed, 116 citations in OpenAlex.
- Ebselen restores mitochondrial function through metabolic rewiring in Barth syndrome and related mitochondrial diseases.EMBO molecular medicine · 2026Article
- HIV capsid inhibitors: Mechanisms, resistance, and therapeutic advances.PLoS pathogens · 2026Review
- Establishment of a green fluorescent protein (GFP)-based reporter for picornaviral 3C proteases.Journal of virology · 2026Article
- Broad-spectrum antiviral activity of ebselen.Scientific reports · 2025Article
- Exploiting the chikungunya virus capsid protein: a focused target for antiviral therapeutic development.Archives of virology · 2025Review
- Unveiling the antiviral inhibitory activity of ebselen and ebsulfur derivatives on SARS-CoV-2 using machine learning-based QSAR, LB-PaCS-MD, and experimental assay.Scientific reports · 2025Article
- Screening of RNA methyltransferase NSP16 inhibitors against SARS-CoV-2 coronavirus and study of related mechanisms.American journal of translational research · 2025Article
- New insights in the mechanism of the SARS-CoV-2 MScientific reports · 2024Article
- Following the Trace of Cyclodextrins on the Selenium and Tellurium Odyssey.International journal of molecular sciences · 2024Review
- Identification of clickable HIV-1 capsid-targeting probes for viral replication inhibition.Cell chemical biology · 2024Article
- Effect of ionic strength on the assembly of simian vacuolating virus capsid protein around poly(styrene sulfonate).The European physical journal. E, Soft matter · 2023Article
- Antiviral Effect of 5'-Arylchalcogeno-3-aminothymidine Derivatives in SARS-CoV-2 Infection.Molecules (Basel, Switzerland) · 2023Article
- Ebselen derivatives inhibit SARS-CoV-2 replication by inhibition of its essential proteins: PLScientific reports · 2023Article
- Ebselen inhibits enterovirus A71-induced apoptosis through reactive oxygen species-mediated signaling pathway.Molecular biology reports · 2023Article
- A Broad-Spectrum Antiviral Molecule, Protoporphyrin IX, Acts as a Moderator of HIV-1 Capsid Assembly by Targeting the Capsid Hexamer.Microbiology spectrum · 2023Article
- Synthesis of Selenoesters via Aldol Condensation and/or Conjugate Reduction and Their Antiviral Activities.ACS omega · 2023Article
- Low-molecular-weight anti-HIV-1 agents targeting HIV-1 capsid proteins.RSC advances · 2023Article
- Modulation of HIV-1 capsid multimerization by sennoside A and sennoside B via interaction with the NTD/CTD interface in capsid hexamer.Frontiers in microbiology · 2023Article
- Specific Interaction of DARPin with HIV-1 CAViruses · 2022Article
- Review
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Authors and funding
19 authors at 4 institutions in 2 countries.
Funding
Abstract
The human immunodeficiency virus type 1 (HIV-1) capsid plays crucial roles in HIV-1 replication and thus represents an excellent drug target. We developed a high-throughput screening method based on a time-resolved fluorescence resonance energy transfer (HTS-TR-FRET) assay, using the C-terminal domain (CTD) of HIV-1 capsid to identify inhibitors of capsid dimerization. This assay was used to screen a library of pharmacologically active compounds, composed of 1,280in vivo-active drugs, and identified ebselen [2-phenyl-1,2-benzisoselenazol-3(2H)-one], an organoselenium compound, as an inhibitor of HIV-1 capsid CTD dimerization. Nuclear magnetic resonance (NMR) spectroscopic analysis confirmed the direct interaction of ebselen with the HIV-1 capsid CTD and dimer dissociation when ebselen is in 2-fold molar excess. Electrospray ionization mass spectrometry revealed that ebselen covalently binds the HIV-1 capsid CTD, likely via a selenylsulfide linkage with Cys198 and Cys218. This compound presents anti-HIV activity in single and multiple rounds of infection in permissive cell lines as well as in primary peripheral blood mononuclear cells. Ebselen inhibits early viral postentry events of the HIV-1 life cycle by impairing the incoming capsid uncoating process. This compound also blocks infection of other retroviruses, such as Moloney murine leukemia virus and simian immunodeficiency virus, but displays no inhibitory activity against hepatitis C and influenza viruses. This study reports the use of TR-FRET screening to successfully identify a novel capsid inhibitor, ebselen, validating HIV-1 capsid as a promising target for drug development.
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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.