ArticleScientific reports2020
Celastrol inhibits ezrin-mediated migration of hepatocellular carcinoma cells.
Article in Scientific reports, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 28 citations in OpenAlex.
- The Antitumor Potential of Celastrol: Research Progress on Antitumor Mechanisms and Strategies for Toxicity Reduction with Efficacy Enhancement.Biomolecules · 2026Review
- How Traditional Chinese Medicine Works: Biological Mechanisms and Clinical Evidence for Hepatocellular Carcinoma Treatment.Drug design, development and therapy · 2026Review
- Traditional Chinese medicine in liver cancer: a visualization and bibliometric analysis.Future science OA · 2025Article
- Akt-elicited phosphorylation of Acapin steers cell migration.Journal of molecular cell biology · 2025Article
- Unveiling the Potential Binding Targets of Celastrol in Colorectal Cancer: A Proteomic Profiling Approach Integrating Cellular Thermal Shift Assay and Pulse Proteolysis.Journal of proteome research · 2025Article
- Celastrol targets CKB-mediated futile creatine cycle in human brown adipocytes thermogenesis.Metabolism open · 2025Article
- Cardiac protection of wogonin in mice with pulmonary fibrosis by regulating Sirt1/ γ-H2AX pathway.Frontiers in pharmacology · 2025Article
- Complex Inhibitory Activity of Pentacyclic Triterpenoids against Cutaneous Melanoma In Vitro and In Vivo: A Literature Review and Reconstruction of Their Melanoma-Related Protein Interactome.ACS pharmacology & translational science · 2024Review
- Review
- Celastrol alleviates atopic dermatitis by regulating Ezrin-mediated mitochondrial fission and fusion.Journal of cellular and molecular medicine · 2024Article
- Recent advances in drug delivery of celastrol for enhancing efficiency and reducing the toxicity.Frontiers in pharmacology · 2024Review
- Mechanistic engineering of celastrol liposomes induces ferroptosis and apoptosis by directly targeting VDAC2 in hepatocellular carcinoma.Asian journal of pharmaceutical sciences · 2023Article
- Article
- SHP2 inhibition improves celastrol-induced growth suppression of colorectal cancer.Frontiers in pharmacology · 2022Article
- SLC7A11/GPX4 Inactivation-Mediated Ferroptosis Contributes to the Pathogenesis of Triptolide-Induced Cardiotoxicity.Oxidative medicine and cellular longevity · 2022Article
- Celastrol: An Update on Its Hepatoprotective Properties and the Linked Molecular Mechanisms.Frontiers in pharmacology · 2022Review
- Nanotechnology-Based Celastrol Formulations and Their Therapeutic Applications.Frontiers in pharmacology · 2021Review
Corrections and comments
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Authors and funding
18 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Progression of hepatocellular carcinoma involves multiple genetic and epigenetic alterations that promote cancer invasion and metastasis. Our recent study revealed that hyperphosphorylation of ezrin promotes intrahepatic metastasis in vivo and cell migration in vitro. Celastrol is a natural product from traditional Chinese medicine which has been used in treating liver cancer. However, the mechanism of action underlying celastrol treatment was less clear. Here we show that ROCK2 is a novel target of celastrol and inhibition of ROCK2 suppresses elicited ezrin activation and liver cancer cell migration. Using cell monolayer wound healing, we carried out a phenotype-based screen of natural products and discovered the efficacy of celastrol in inhibiting cell migration. The molecular target of celastrol was identified as ROCK2 using celastrol affinity pull-down assay. Our molecular docking analyses indicated celastrol binds to the active site of ROCK2 kinase. Mechanistically, celastrol inhibits the ROCK2-mediated phosphorylation of ezrin at Thr567 which harnesses liver cancer cell migration. Our findings suggest that targeting ROCK2-ezrin signaling is a potential therapeutic niche for celastrol-based intervention of cancer progression in hepatocellular carcinoma.
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