ArticleNature communications2016
Ailanthone targets p23 to overcome MDV3100 resistance in castration-resistant prostate cancer.
Article in Nature communications, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 51 papers.
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Who cites it
51 citing papers in PubMed, 109 citations in OpenAlex.
- Nuclear prostaglandin E synthase 3 promotes hepatocellular carcinoma growth with immunosuppressive macrophage polarization via the SP1/TGF-β axis.Molecular biomedicine · 2026Article
- Ailanthone restrains hepatocellular carcinoma progression by inducing ferroptosis and disrupting mitochondrial homeostasis.Scientific reports · 2025Article
- Ailanthone induces triple-negative breast cancer cells death involving the inhibition of OTUB1-mediated ERRα deubiquitylation.Journal of advanced research · 2025Article
- RBM14 enhances transcriptional activity of p23 regulating CXCL1 expression to induce lung cancer metastasis.Acta pharmaceutica Sinica. B · 2025Article
- Article
- Quassinoids as Promising Anti-cancer Agents.Current medicinal chemistry · 2025Review
- Ailanthone induces apoptosis in U-2OS cells through the endoplasmic reticulum stress.Frontiers in immunology · 2025Article
- Androgen receptor activation promotes tumor progression in canine and human triple negative breast cancer cell lines.Frontiers in veterinary science · 2025Article
- Ailanthone ameliorates pulmonary fibrosis by suppressing JUN-dependent MEOX1 activation.Acta pharmaceutica Sinica. B · 2024Article
- FRET Assays for the Identification ofPharmaceuticals (Basel, Switzerland) · 2024Article
- MiR26a reverses enzalutamide resistance in a bone-tumor targeted system with an enhanced effect on bone metastatic CRPC.Journal of nanobiotechnology · 2024Article
- Ailanthone blocks mitophagy to promote mtDNA leakage through BAX-BAK1 pores and suppress hepatocellular carcinoma cell proliferation.Frontiers in pharmacology · 2024Article
- Elucidation of the mechanism of action of ailanthone in the treatment of colorectal cancer: integration of network pharmacology, bioinformatics analysis and experimental validation.Frontiers in pharmacology · 2024Article
- Targeting of STAT5 using the small molecule topotecan hydrochloride suppresses acute myeloid leukemia progression.Oncology reports · 2023Article
- ASFV transcription reporter screening system identifies ailanthone as a broad antiviral compound.Virologica Sinica · 2023Article
- The crosstalk between ubiquitination and endocrine therapy.Journal of molecular medicine (Berlin, Germany) · 2023Review
- Article
- Comprehensive pan-cancer analysis of PTGES3 and its prognostic role in hepatocellular carcinoma.Frontiers in oncology · 2023Article
- The traditional chinese medicine monomer Ailanthone improves the therapeutic efficacy of anti-PD-L1 in melanoma cells by targeting c-Jun.Journal of experimental & clinical cancer research : CR · 2022Article
- Isobavachalcone's Alleviation of Pyroptosis Contributes to Enhanced Apoptosis in Glioblastoma: Possible Involvement of NLRP3.Molecular neurobiology · 2022Article
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14 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Androgen receptor (AR) antagonist MDV3100 is the first therapeutic approach in treating castration-resistant prostate cancer (CRPC), but tumours frequently become drug resistant via multiple mechanisms including AR amplification and mutation. Here we identify the small molecule Ailanthone (AIL) as a potent inhibitor of both full-length AR (AR-FL) and constitutively active truncated AR splice variants (AR-Vs). AIL binds to the co-chaperone protein p23 and prevents AR's interaction with HSP90, thus resulting in the disruption of the AR-chaperone complex followed by ubiquitin/proteasome-mediated degradation of AR as well as other p23 clients including AKT and Cdk4, and downregulates AR and its target genes in PCa cell lines and orthotopic animal tumours. In addition, AIL blocks tumour growth and metastasis of CRPC. Finally, AIL possesses favourable drug-like properties such as good bioavailability, high solubility, lack of CYP inhibition and low hepatotoxicity. In general, AIL is a potential candidate for the treatment of CRPC.
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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.