Histone Deacetylase Inhibitors

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  Subject Areas on Research

  • A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold. 
  • A phase 1 trial of the oral DNA methyltransferase inhibitor CC-486 and the histone deacetylase inhibitor romidepsin in advanced solid tumors. 
  • A phase 2 study of mocetinostat, a histone deacetylase inhibitor, in relapsed or refractory lymphoma. 
  • A phase I study of panobinostat in pediatric patients with refractory solid tumors, including CNS tumors. 
  • A precision oncology approach to the pharmacological targeting of mechanistic dependencies in neuroendocrine tumors. 
  • Aggresome disruption: a novel strategy to enhance bortezomib-induced apoptosis in pancreatic cancer cells. 
  • An overview of naturally occurring histone deacetylase inhibitors. 
  • Anticolon cancer activity of largazole, a marine-derived tunable histone deacetylase inhibitor. 
  • Comparison of the prognostic utility of the revised International Prognostic Scoring System and the French Prognostic Scoring System in azacitidine-treated patients with myelodysplastic syndromes. 
  • Concept of histone deacetylases in cancer: Reflections on esophageal carcinogenesis and treatment. 
  • Cyclophilin A and Ess1 interact with and regulate silencing by the Sin3-Rpd3 histone deacetylase. 
  • Deactylase inhibitors disrupt cellular complexes containing protein phosphatases and deacetylases. 
  • Differential effects of prostate cancer therapeutics on neuroendocrine transdifferentiation. 
  • Discovery of a fluorescent probe with HDAC6 selective inhibition. 
  • Effects of downregulated HDAC6 expression on the proliferation of lung cancer cells. 
  • Epigenetic therapy for solid tumors: from bench science to clinical trials. 
  • Evaluation of class I HDAC isoform selectivity of largazole analogues. 
  • Evaluation of the long-term tolerability and clinical benefit of vorinostat in patients with advanced cutaneous T-cell lymphoma. 
  • FOXO transcription factors control E2F1 transcriptional specificity and apoptotic function. 
  • Glucocorticoids and histone deacetylase inhibitors cooperate to block the invasiveness of basal-like breast cancer cells through novel mechanisms. 
  • Glucose metabolism as a target of histone deacetylase inhibitors. 
  • HDAC6 modulates cell motility by altering the acetylation level of cortactin. 
  • HDACs in skeletal muscle remodeling and neuromuscular disease. 
  • Histone Deacetylase 3 Inhibition Overcomes BIM Deletion Polymorphism-Mediated Osimertinib Resistance in EGFR-Mutant Lung Cancer. 
  • Histone Deacetylase Inhibitors Inhibit Rhabdomyosarcoma by Reactive Oxygen Species-Dependent Targeting of Specificity Protein Transcription Factors. 
  • Histone Deacetylase Inhibitors: An Attractive Therapeutic Strategy Against Breast Cancer. 
  • Histone deacetylase 3 binds to and regulates the GCMa transcription factor. 
  • Histone deacetylase inhibitor panobinostat induces clinical responses with associated alterations in gene expression profiles in cutaneous T-cell lymphoma. 
  • Histone deacetylase inhibitors in hepatocellular carcinoma: A therapeutic perspective. 
  • Histone deacetylation critically determines T cell subset radiosensitivity. 
  • Identification of a cancer stem cell-specific function for the histone deacetylases, HDAC1 and HDAC7, in breast and ovarian cancer. 
  • Imprinted CDKN1C is a tumor suppressor in rhabdoid tumor and activated by restoration of SMARCB1 and histone deacetylase inhibitors. 
  • Inhibitors of histone deacetylases promote hematopoietic stem cell self-renewal. 
  • Interleukin-15-Stimulated Natural Killer Cells Clear HIV-1-Infected Cells following Latency Reversal Ex Vivo. 
  • Intracellular trafficking of histone deacetylase 4 regulates neuronal cell death. 
  • Largazole pharmacokinetics in rats by LC-MS/MS. 
  • Largazole: from discovery to broad-spectrum therapy. 
  • Latency reversal and viral clearance to cure HIV-1. 
  • Lipids Reprogram Metabolism to Become a Major Carbon Source for Histone Acetylation. 
  • Loss of betaglycan expression in ovarian cancer: role in motility and invasion. 
  • Low-Dose Histone Deacetylase Inhibitor Treatment Leads to Tumor Growth Arrest and Multi-Lineage Differentiation of Malignant Rhabdoid Tumors. 
  • Lunasin does not slow ALS progression: results of an open-label, single-center, hybrid-virtual 12-month trial. 
  • Mechanism-Based Inhibitors of the Human Sirtuin 5 Deacylase: Structure-Activity Relationship, Biostructural, and Kinetic Insight. 
  • Methods for the analysis of histone H3 and H4 acetylation in blood. 
  • Nanoparticles for urothelium penetration and delivery of the histone deacetylase inhibitor belinostat for treatment of bladder cancer. 
  • Panobinostat for the management of multiple myeloma. 
  • Phase 2 study of sodium phenylbutyrate in ALS. 
  • Phase I/II study of mocetinostat in combination with gemcitabine for patients with advanced pancreatic cancer and other advanced solid tumors. 
  • Phosphorus-based SAHA analogues as histone deacetylase inhibitors. 
  • Promoter methylation and silencing of the tissue factor pathway inhibitor-2 (TFPI-2), a gene encoding an inhibitor of matrix metalloproteinases in human glioma cells. 
  • Psammaplin A as a general activator of cell-based signaling assays via HDAC inhibition and studies on some bromotyrosine derivatives. 
  • QT interval prolongation and torsades de pointes in a patient undergoing treatment with vorinostat: a case report and review of the literature. 
  • Regulation of p53 by hypoxia: dissociation of transcriptional repression and apoptosis from p53-dependent transactivation. 
  • Restoration of the cystic fibrosis transmembrane conductance regulator function by splicing modulation. 
  • Short-chain fatty acids enhance nuclear receptor activity through mitogen-activated protein kinase activation and histone deacetylase inhibition. 
  • Suppression of oxidative stress by β-hydroxybutyrate, an endogenous histone deacetylase inhibitor. 
  • Synthesis and activity of largazole analogues with linker and macrocycle modification. 
  • Synthesis and biological evaluation of largazole zinc-binding group analogs. 
  • Sézary syndrome: immunopathogenesis, literature review of therapeutic options, and recommendations for therapy by the United States Cutaneous Lymphoma Consortium (USCLC). 
  • The HDAC inhibitor SB939 overcomes resistance to BCR-ABL kinase Inhibitors conferred by the BIM deletion polymorphism in chronic myeloid leukemia. 
  • The class I HDAC inhibitor MGCD0103 induces cell cycle arrest and apoptosis in colon cancer initiating cells by upregulating Dickkopf-1 and non-canonical Wnt signaling. 
  • The cytoplasmic deacetylase HDAC6 is required for efficient oncogenic tumorigenesis. 
  • The discovery of histone deacetylase. 
  • The histone deacetylase inhibitor trichostatin a decreases lymphangiogenesis by inducing apoptosis and cell cycle arrest via p21-dependent pathways. 
  • The synergistic combination of the farnesyl transferase inhibitor lonafarnib and paclitaxel enhances tubulin acetylation and requires a functional tubulin deacetylase. 
  • Timing of valproic acid in acute lung injury: prevention is the best therapy? 
  • Total synthesis and molecular target of largazole, a histone deacetylase inhibitor. 
  • Validation of histone deacetylase 3 as a therapeutic target in castration-resistant prostate cancer. 
  • Valproic acid without intensified antiviral therapy has limited impact on persistent HIV infection of resting CD4+ T cells. 
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  Keywords of People

  • Hirschey, Matthew, Associate Professor, Pharmacology & Cancer Biology
  • McDonnell, Donald Patrick, Glaxo-Wellcome Distinguished Professor of Molecular Cancer Biology, in the School of Medicine, Duke Innovation & Entrepreneurship