ArticleJournal of molecular biology2011
Celastrol inhibits Tat-mediated human immunodeficiency virus (HIV) transcription and replication.
Article in Journal of molecular biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 56 citations in OpenAlex.
- Advancing Antiviral Design: Integrating Natural Products, Computation and Targeted Delivery.Chemical biology & drug design · 2026Review
- Celastrol Inhibits Porcine Epidemic Diarrhea Virus Replication by Promoting ROS-Mediated Apoptosis.Transboundary and emerging diseases · 2025Article
- Review
- Synthesis and anticancer properties of celastrol derivatives involved in the inhibition of VEGF.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Celastrol attenuates hepatitis C virus translation and inflammatory response in mice by suppressing heat shock protein 90β.Acta pharmacologica Sinica · 2023Article
- 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
- Article
- Michael acceptor molecules in natural products and their mechanism of action.Frontiers in pharmacology · 2022Review
- Modulation of Inflammation-Related Lipid Mediator Pathways by Celastrol During Human Macrophage Polarization.Journal of inflammation research · 2022Article
- Conformational dynamics and energetics of viral RNA recognition by lab-evolved proteins.Physical chemistry chemical physics : PCCP · 2021Article
- Will curcumin nanosystems be the next promising antiviral alternatives in COVID-19 treatment trials?Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2021Review
- Bioactive Terpenes and Their Derivatives as Potential SARS-CoV-2 Proteases Inhibitors from Molecular Modeling Studies.Biomolecules · 2021Article
- Identification of celastrol as a novel HIV-1 latency reversal agent by an image-based screen.PloS one · 2021Article
- Interrelated Mechanism by Which the Methide Quinone Celastrol, Obtained from the Roots ofInternational journal of molecular sciences · 2020Article
- Recent advances in natural anti-HIV triterpenoids and analogs.Medicinal research reviews · 2020Review
- The Emerging Therapeutic Potential of Nitro Fatty Acids and Other Michael Acceptor-Containing Drugs for the Treatment of Inflammation and Cancer.Frontiers in pharmacology · 2020Review
- Face-time with TAR: Portraits of an HIV-1 RNA with diverse modes of effector recognition relevant for drug discovery.The Journal of biological chemistry · 2019Review
- Current Strategies for Elimination of HIV-1 Latent Reservoirs Using Chemical Compounds Targeting Host and Viral Factors.AIDS research and human retroviruses · 2019Review
- Celastrol inhibits colon cancer cell proliferation by downregulating miR-21 and PI3K/AKT/GSK-3β pathway.International journal of clinical and experimental pathology · 2019Article
- Synergic effect of curcumin and its structural analogue (Monoacetylcurcumin) on anti-influenza virus infection.Journal of food and drug analysis · 2018Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Current drugs used for antiretroviral therapy against human immunodeficiency virus (HIV) have a narrow spectrum of activity and, more often, have associated toxicities and severe side effects in addition to developing resistance. Thus, there is a need to develop new therapeutic strategies against HIV/AIDS to complement the already existing ones. Surprisingly, transactivator of transcription (Tat), an early virus-encoded protein required for the efficient transcription of the HIV genome, has not been developed as a target for small molecular therapeutics. We have previously described the ability of an endogenous Michael acceptor electrophile (MAE), 15-deoxy-Δ(12,14)-prostaglandin J(2) (15d-PGJ(2)), to inhibit Tat-dependent transcription by targeting its cysteine (Cys)-rich domain. In an effort to identify other MAEs possessing inhibitory activity against HIV-1 Tat, we tested a collection of plant-derived compounds with electrophilic properties, including curcumin, rosmarinic acid, and gambogic acid, for their ability to inhibit Tat. Celastrol (Cel), a triterpenoid MAE isolated from Tripterygium wilfordii, exhibited the highest inhibitory activity against Tat. Using biochemical techniques, we demonstrate that Cel, by covalently modifying the cysteine thiols, inhibits Tat transactivation function. Using circular dichroism spectroscopy, we show that alkylation of Tat brought about a change in the secondary structure of Tat, which inhibited the transcription elongation of the HIV proviral genome by effecting mechanisms other than Tat-TAR (transactivation-responsive region) interaction. Our results demonstrate the underlying mechanism of antiretroviral activity of the plant-derived MAEs and suggest that Cel could serve as a lead compound to develop novel antiviral therapeutics.
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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.