ArticleJournal of enzyme inhibition and medicinal chemistry2020
The selenium-containing drug ebselen potently disrupts LEDGF/p75-HIV-1 integrase interaction by targeting LEDGF/p75.
Article in Journal of enzyme inhibition and medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 32 citations in OpenAlex.
- HIV capsid inhibitors: Mechanisms, resistance, and therapeutic advances.PLoS pathogens · 2026Review
- Block-and-Lock Approaches for HIV Cure: Mechanistic Insights, Challenges, and Emerging Role of CPSF6.International journal of molecular sciences · 2026Review
- Following the Trace of Cyclodextrins on the Selenium and Tellurium Odyssey.International journal of molecular sciences · 2024Review
- COVID-19 therapeutics: Clinical application of repurposed drugs and futuristic strategies for target-based drug discovery.Genes & diseases · 2023Review
- Synthesis of Selenoesters via Aldol Condensation and/or Conjugate Reduction and Their Antiviral Activities.ACS omega · 2023Article
- Chemoselective Preparation of New Families of Phenolic-Organoselenium Hybrids-A Biological Assessment.Molecules (Basel, Switzerland) · 2022Article
- Advances in the computational landscape for repurposed drugs against COVID-19.Drug discovery today · 2021Review
- Ebselen and Analogues: Pharmacological Properties and Synthetic Strategies for Their Preparation.Molecules (Basel, Switzerland) · 2021Review
- Isoselenocyanates: Synthesis and Their Use for Preparing Selenium-Based Heterocycles.Synthesis · 2021Article
- Toxicology and pharmacology of synthetic organoselenium compounds: an update.Archives of toxicology · 2021Review
- Drug Repurposing Approach, Potential Drugs, and Novel Drug Targets for COVID-19 Treatment.Journal of environmental and public health · 2021Review
- LEDGINs, Inhibitors of the Interaction Between HIV-1 Integrase and LEDGF/p75, Are Potent Antivirals with a Potential to Cure HIV Infection.Advances in experimental medicine and biology · 2021Article
- Ebselen, a new candidate therapeutic against SARS-CoV-2.International journal of surgery (London, England) · 2020Article
- Selenium and selenoproteins in viral infection with potential relevance to COVID-19.Redox biology · 2020Review
- Potential therapeutic use of ebselen for COVID-19 and other respiratory viral infections.Free radical biology & medicine · 2020Review
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Lens-epithelium-derived growth-factor (LEDGF/p75)-binding site on HIV-1 integrase (IN), is an attractive target for antiviral chemotherapy. Small-molecule compounds binding to this site are referred as LEDGF-IN inhibitors (LEDGINs). In this study, compound libraries were screened to identify new inhibitors of LEDGF/p75-IN interaction. Ebselen (2-phenyl-1,2-benzisoselenazol-3-one), a reported anti-HIV-1 agent, was identified as a moderate micromolar inhibitor of LEDGF/p75-IN interaction. Ebselen inhibited the interaction by binding to LEDGF/p75 and the ability of ebselen to inhibit the interaction could be reversed by dithiothreitol (DTT). BLI experiment showed that ebselen probably formed selenium-sulphur bonds with reduced thiols in LEDGF/p75. To the best of our knowledge, we showed for the first time that small-molecule compound, ebselen inhibited LEDGF/p75-IN interaction by directly binding to LEDGF/p75. The compound discovered here could be used as probe compounds to design and develop new disrupter of LEDGF/p75-IN interaction.
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