ArticleBreast cancer research and treatment2016
Selective activity of deguelin identifies therapeutic targets for androgen receptor-positive breast cancer.
Article in Breast cancer research and treatment, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
25 citing papers in PubMed, 45 citations in OpenAlex.
- Looking beyond the ER, PR, and HER2: what's new in the ARsenal for combating breast cancer?Reproductive biology and endocrinology : RB&E · 2025Review
- Deguelin's Anticancer Bioactivity: Challenges and Opportunities in Medicinal Chemistry.Frontiers in pharmacology · 2025Review
- HDAC inhibitors target IRS4 to enhance anti‑AR therapy in AR‑positive triple‑negative breast cancer.International journal of oncology · 2024Article
- Potential Therapeutic Targets for Luminal Androgen Receptor Breast Cancer: What We Know so Far.OncoTargets and therapy · 2023Review
- Emergence of Nanotechnology as a Powerful Cavalry against Triple-Negative Breast Cancer (TNBC).Pharmaceuticals (Basel, Switzerland) · 2022Review
- Article
- Therapeutic Strategies for Metastatic Triple-Negative Breast Cancers: From Negative to Positive.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Review
- An Integrated Strategy for the Detection, Dereplication, and Identification of DNA-Binding Biomolecules from Complex Natural Product Mixtures.Journal of natural products · 2021Article
- Clinicopathological Features and Treatment Challenges in Triple Negative Breast Cancer Patients: A Retrospective Cohort Study.Turk patoloji dergisi · 2021Article
- CRISPR-Cas9 Genome-Wide Knockout Screen Identifies Mechanism of Selective Activity of Dehydrofalcarinol in Mesenchymal Stem-like Triple-Negative Breast Cancer Cells.Journal of natural products · 2020Article
- An Electrophilic Deguelin Analogue Inhibits STAT3 Signaling in H-Biomedicines · 2020Article
- Triple-Negative Breast Cancer Cells Exhibit Differential Sensitivity to Cardenolides fromJournal of natural products · 2020Article
- Leucinostatins fromJournal of natural products · 2020Article
- G-MDSCs-Derived Exosomal miRNA-143-3p Promotes Proliferation via Targeting of ITM2B in Lung Cancer.OncoTargets and therapy · 2020Article
- Anticancer Effects of Constituents of Herbs Targeting Osteosarcoma.Chinese journal of integrative medicine · 2019Review
- Anti-tumor activity of BET inhibitors in androgen-receptor-expressing triple-negative breast cancer.Scientific reports · 2019Article
- Triple-negative breast cancer cell line sensitivity to englerin A identifies a new, targetable subtype.Breast cancer research and treatment · 2019Article
- The Natural Flavonoid Compound Deguelin Inhibits HCMV Lytic Replication within Fibroblasts.Viruses · 2018Article
- The "Yin and Yang" of Natural Compounds in Anticancer Therapy of Triple-Negative Breast Cancers.Cancers · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Triple-negative breast cancers (TNBC) are aggressive malignancies with no effective targeted therapies. Recent gene expression profiling of these heterogeneous cancers and the classification of cell line models now allows for the identification of compounds with selective activities against molecular subtypes of TNBC. The natural product deguelin was found to have selective activity against MDA-MB-453 and SUM-185PE cell lines, which both model the luminal androgen receptor (LAR) subtype of TNBC. Deguelin potently inhibited proliferation of these cells with GI50 values of 30 and 61 nM, in MDA-MB-453 and SUM-185PE cells, respectively. Deguelin had exceptionally high selectivity, 197 to 566-fold, for these cell lines compared to cell lines representing other TNBC subtypes. Deguelin's mechanisms of action were investigated to determine how it produced these potent and selective effects. Our results show that deguelin has dual activities, inhibiting PI3K/Akt/mTOR signaling, and decreasing androgen receptor levels and nuclear localization. Based on these data, we hypothesized that the combination of the mTOR inhibitor rapamycin and the antiandrogen enzalutamide would have efficacy in LAR models. Rapamycin and enzalutamide showed additive effects in MDA-MB-453 cells, and both drugs had potent antitumor efficacy in a LAR xenograft model. These results suggest that the combination of antiandrogens and mTOR inhibitors might be an effective strategy for the treatment of androgen receptor-expressing TNBC.
Indexed as
Identifiers
What OpenQuestion holds
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.