Abstract
Histone deacetylase (HDAC) inhibitors constitute a novel and growing class of anticancer agents that function by altering intracellular patterns of histone acetylation, the so-called epigenetic “histone code,” thereby producing changes in cell cycle arrest, differentiation, and/or apoptosis in tumor cells. This overview describes the chemistry and preliminary characterization of recently disclosed molecules in three major classes of HDAC inhibitors: hydroxamic acids, 2-aminobenzanilides, and cyclic peptides. In addition, results from recent clinical trials on isotype-selective HDAC inhibitors are reviewed. It is clear from the plethora of new molecules and the encouraging results from clinical trials that HDAC inhibitors hold a great deal of promise, particularly as add-on therapy, for the treatment of a variety of solid and hematologic cancers.
Keywords: Acetylation, antineoplastic agent, clinical trials, histone deacetylases, histones, apoptosis, cell-cycle arrest
Current Topics in Medicinal Chemistry
Title: Histone Deacetylase Inhibitors in Cancer Therapy: New Compounds and Clinical Update of Benzamide-Type Agents
Volume: 8 Issue: 10
Author(s): Oscar Moradei, Arkadii Vaisburg and Robert E. Martell
Affiliation:
Keywords: Acetylation, antineoplastic agent, clinical trials, histone deacetylases, histones, apoptosis, cell-cycle arrest
Abstract: Histone deacetylase (HDAC) inhibitors constitute a novel and growing class of anticancer agents that function by altering intracellular patterns of histone acetylation, the so-called epigenetic “histone code,” thereby producing changes in cell cycle arrest, differentiation, and/or apoptosis in tumor cells. This overview describes the chemistry and preliminary characterization of recently disclosed molecules in three major classes of HDAC inhibitors: hydroxamic acids, 2-aminobenzanilides, and cyclic peptides. In addition, results from recent clinical trials on isotype-selective HDAC inhibitors are reviewed. It is clear from the plethora of new molecules and the encouraging results from clinical trials that HDAC inhibitors hold a great deal of promise, particularly as add-on therapy, for the treatment of a variety of solid and hematologic cancers.
Export Options
About this article
Cite this article as:
Moradei Oscar, Vaisburg Arkadii and Martell E. Robert, Histone Deacetylase Inhibitors in Cancer Therapy: New Compounds and Clinical Update of Benzamide-Type Agents, Current Topics in Medicinal Chemistry 2008; 8 (10) . https://dx.doi.org/10.2174/156802608784911581
DOI https://dx.doi.org/10.2174/156802608784911581 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |

- Author Guidelines
- Bentham Author Support Services (BASS)
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Chitosan Nano-encapsulation Enhances Gedunin Cytotoxicity A gainst Human Non-small-cell Lung Cancer (NCI-H292) Cell Line
Drug Delivery Letters Redox Signaling Pathways Involved in Neuronal Ischemic Preconditioning
Current Neuropharmacology Small-molecule Inhibitors of Fibroblast Growth Factor Receptor (FGFR) Tyrosine Kinases (TK)
Current Pharmaceutical Design Lycopene: A Review of Its Potential as an Anticancer Agent
Current Medicinal Chemistry - Anti-Cancer Agents Carotenoids as Modulators of Intracellular Signaling Pathways
Current Signal Transduction Therapy The Pharmacological Pathways of GnRH Mediating the Inhibition of Mammary Tumours: Implications in Humans and Domestic Animals
Current Medicinal Chemistry Perspectives On Membrane-associated Progesterone Receptors As Prospective Therapeutic Targets
Current Drug Targets Effects of Estrogens on Atherogenesis
Current Vascular Pharmacology PI3K/Akt/JNK/c-Jun Signaling Pathway is a Mediator for Arsenite- Induced Cyclin D1 Expression and Cell Growth in Human Bronchial Epithelial Cells
Current Cancer Drug Targets Osteoporosis in Patients with Breast and Prostate Cancer: Effect of Disease and Treatment Modalities
Endocrine, Metabolic & Immune Disorders - Drug Targets Hyperandrogenism, Insulin Resistance and Hyperinsulinemia as Cardiovascular Risk Factors in Diabetes Mellitus
Current Diabetes Reviews Prolyl-Specific Peptidases and Their Inhibitors in Biological Processes
Current Chemical Biology Role of Platelets in Angiogenesis in Health and Disease
Current Angiogenesis (Discontinued) Multi-Targeted Histone Deacetylase Inhibitors in Cancer Therapy
Current Medicinal Chemistry Decoding the Knots of Initiation of Oncogenic Epithelial-Mesenchymal Transition in Tumor Progression
Current Cancer Drug Targets A Molecular Link Between Diabetes and Breast Cancer: Therapeutic Potential of Repurposing Incretin-based Therapies for Breast Cancer
Current Cancer Drug Targets Editorial [Hot Topic: Surgical Treatment of Endometrial Cancer (Guest Editor: Maite Cusido Gimferrer)]
Current Women`s Health Reviews Bone Disease - Current Knowledge and Future Prospects
Current Genomics Reversal of Bone Cancer Pain by HSV-1-Mediated Silencing of CNTF in an Afferent Area of the Spinal Cord Associated with AKT-ERK Signal Inhibition
Current Gene Therapy Glioma: Tryptophan Catabolite and Melatoninergic Pathways Link microRNA, 14-3- 3, Chromosome 4q35, Epigenetic Processes and other Glioma Biochemical Changes
Current Pharmaceutical Design