ArticleProceedings of the National Academy of Sciences of the United States of America2010
The HDAC inhibitor LBH589 (panobinostat) is an inhibitory modulator of aromatase gene expression.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 56 citations in OpenAlex.
- Nucleic sexual hormone receptor signaling pathways in breast cancer: function regulation, crosstalk, and therapeutic implications.NPJ precision oncology · 2026Review
- Steroidogenic Acute Regulatory Protein in Breast Cancer: Mechanistic Insights into Pathogenesis and Therapeutics.International journal of molecular sciences · 2026Review
- FAME-CRISPR improves CRISPR-Cas9 genome editing via HDAC inhibition and engineered virus-like particle delivery.Cell reports methods · 2026Article
- Histone acetylation modulators in breast cancer.Breast cancer research : BCR · 2025Review
- Estrogen Receptor Signaling in Breast Cancer.Cancers · 2023Review
- Inhibition of histone deacetylases attenuates tumor progression and improves immunotherapy in breast cancer.Frontiers in immunology · 2023Review
- Hormonal and Genetic Regulatory Events in Breast Cancer and Its Therapeutics: Importance of the Steroidogenic Acute Regulatory Protein.Biomedicines · 2022Review
- Type I IFN stimulates IFI16-mediated aromatase expression in adipocytes that promotes ECellular and molecular life sciences : CMLS · 2022Article
- Potential of histone deacetylase inhibitors in the control and regulation of prostate, breast and ovarian cancer.Frontiers in chemistry · 2022Review
- Regulation of Estradiol Synthesis by Aromatase Interacting Partner in Breast (AIPB).Molecular and cellular biology · 2021Article
- Panobinostat penetrates the blood-brain barrier and achieves effective brain concentrations in a murine model.Cancer chemotherapy and pharmacology · 2021Article
- Preclinical evaluation of exemestane as a novel chemotherapy for gastric cancer.Journal of cellular and molecular medicine · 2019Article
- Overexpression of the steroidogenic acute regulatory protein in breast cancer: Regulation by histone deacetylase inhibition.Biochemical and biophysical research communications · 2019Article
- Novel mediators of breast cancer bone metastasis-insights from studies of gene-regulation and the global proteome.Annals of translational medicine · 2018Article
- Aromatase Acetylation Patterns and Altered Activity in Response to Sirtuin Inhibition.Molecular cancer research : MCR · 2018Article
- The formation of giant plasma membrane vesicles enable new insights into the regulation of cholesterol efflux.Experimental cell research · 2018Article
- Hsp90 and PKM2 Drive the Expression of Aromatase in Li-Fraumeni Syndrome Breast Adipose Stromal Cells.The Journal of biological chemistry · 2016Article
- Targeting breast cancer stem cells in triple-negative breast cancer using a combination of LBH589 and salinomycin.Breast cancer research and treatment · 2015Article
- AroER tri-screen is a biologically relevant assay for endocrine disrupting chemicals modulating the activity of aromatase and/or the estrogen receptor.Toxicological sciences : an official journal of the Society of Toxicology · 2014Article
- Modulation of CYP19 expression by cabbage juices and their active components: indole-3-carbinol and 3,3'-diindolylmethene in human breast epithelial cell lines.European journal of nutrition · 2013Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
Abstract
Aromatase converts androgens to estrogens. Although third-generation aromatase inhibitors (AIs) are important drugs in hormonal therapy for breast cancer in postmenopausal women, there are concerns about the side effects associated with the estrogen deprivation achieved with AIs. Expression of aromatase in breast cancer tissue is driven by different promoters than those in noncancer tissues; thus, suppression of aromatase expression in cancer tissues through the down-regulation of breast tumor-specific promoters would reduce the side effects associated with whole-body suppression of estrogen biosynthesis by AIs. We report that histone deacetylase inhibitor LBH589 (panobinostat) is a potent inhibitor of aromatase expression (with an IC(50) value < 25 nM). LBH589 selectively suppresses human aromatase gene promoters I.3/II, which are preferentially used in breast cancer tissue. Furthermore, using the H295R cell culture model, we found that achieving the same degree of inhibition of aromatase activity required only one-fifth as much letrozole (an AI) in the presence of 25 nM LBH589 as in the absence of LBH589. We also used an H295R/MCF7 coculture model to demonstrate the synergistic interaction of LBH589 + letrozole in suppressing the proliferation of hormone-responsive breast cancer cells. Finally, our results also indicate that LBH589 down-regulates the activity of promoters I.3/II in an epigenetic fashion. LBH589 reduces the levels of C/EBPdelta, decreases the binding of C/EBPdelta, and increases the levels and binding of acetyl-histones to the promoters I.3/II. These findings provide an important basis for future clinical evaluations of LBH589 in hormone-dependent breast cancer.
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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.