Abstract
Histone deacetylases (HDACs) play a central role in the epigenetic regulation of gene expression. Aberrant activity of HDACs has been found in several human cancers leading to the development of HDAC inhibitors (HDACi) as anti-tumors drugs. In fact, over the last years, a number of HDACi have been evaluated in clinical trials; these drugs have the common ability to hyperacetylate both histone and non-histone targets, resulting in a variety of effects on both cancer cells and immune responses. Clinical trials of HDACi conducted in solid tumors and hematological malignancies have shown a better clinical efficacy of these drugs in hematological malignancies. In this review, will be highlighted the mechanisms of action underlying the clinical responses obtained with these drugs and the doubts regarding the use of HDACi in cancer therapy.
Keywords: Histone deacetylases, histone deacetylases inhibitors, hematological malignancies, HDACs, epigenetic, regulation, Aberrant activity, human cancers, inhibitors, HDACi, anti-tumors, hyperacetylate, non-histone
Mini-Reviews in Medicinal Chemistry
Title: Histone Deacetylase Inhibitors in the Treatment of Hematological Malignancies
Volume: 11 Issue: 6
Author(s): A. Petrella, B. Fontanella, A. Carratu, V. Bizzarro, M. Rodriquez and L. Parente
Affiliation:
Keywords: Histone deacetylases, histone deacetylases inhibitors, hematological malignancies, HDACs, epigenetic, regulation, Aberrant activity, human cancers, inhibitors, HDACi, anti-tumors, hyperacetylate, non-histone
Abstract: Histone deacetylases (HDACs) play a central role in the epigenetic regulation of gene expression. Aberrant activity of HDACs has been found in several human cancers leading to the development of HDAC inhibitors (HDACi) as anti-tumors drugs. In fact, over the last years, a number of HDACi have been evaluated in clinical trials; these drugs have the common ability to hyperacetylate both histone and non-histone targets, resulting in a variety of effects on both cancer cells and immune responses. Clinical trials of HDACi conducted in solid tumors and hematological malignancies have shown a better clinical efficacy of these drugs in hematological malignancies. In this review, will be highlighted the mechanisms of action underlying the clinical responses obtained with these drugs and the doubts regarding the use of HDACi in cancer therapy.
Export Options
About this article
Cite this article as:
Petrella A., Fontanella B., Carratu A., Bizzarro V., Rodriquez M. and Parente L., Histone Deacetylase Inhibitors in the Treatment of Hematological Malignancies, Mini-Reviews in Medicinal Chemistry 2011; 11 (6) . https://dx.doi.org/10.2174/138955711795843347
DOI https://dx.doi.org/10.2174/138955711795843347 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...read more
- Author Guidelines
- 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
Related Articles
-
Targeting Rho GTPases by Peptidic Structures
Current Pharmaceutical Design Metabolism of the Novel IMP Dehydrogenase Inhibitor Benzamide Riboside
Current Medicinal Chemistry WT1 Peptide Vaccine as a Paradigm for “Cancer Antigen-Derived Peptide”-Based Immunotherapy for Malignancies: Successful Induction of Anti-Cancer Effect by Vaccination with a Single Kind of WT1 Peptide
Anti-Cancer Agents in Medicinal Chemistry Paclitaxel Formulations: Challenges and Novel Delivery Options
Current Drug Delivery Preliminary Experience with Yttrium-90-labelled Rituximab (Chimeric Anti CD-20 Antibody) in Patients with Relapsed and Refractory B Cell Non-Hodgkins Lymphoma
Current Radiopharmaceuticals CD47 Functionalization of Nanoparticles as a Poly(ethylene glycol) Alternative: A Novel Approach to Improve Drug Delivery
Current Drug Targets Microgravity Alters Cancer Growth and Progression
Current Cancer Drug Targets Soy Isoflavone Alleviates Aβ1-42-Induced Impairment of Learning and Memory Ability Through the Regulation of RAGE/LRP-1 in Neuronal and Vascular Tissue
Current Neurovascular Research Cerebral Artery Signal Transduction Mechanisms: Developmental Changes in Dynamics and Ca<sup>2+</sup> Sensitivity
Current Vascular Pharmacology Management Of Elderly Patients With Diffuse Large B-Cell Lymphomas
Anti-Cancer Agents in Medicinal Chemistry Hepatitis C Virus Infection and Antiviral Treatment in Marginal Zone Lymphomas
Current Clinical Pharmacology Oral Agents in Multiple Sclerosis
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Benzimidazole Derivatives as Kinase Inhibitors
Current Medicinal Chemistry Polyphenols: Biological Activities, Molecular Targets, and the Effect of Methylation
Current Molecular Pharmacology Novel Approaches to Modulate Apoptosis Resistance: Basic and Clinical Implications in the Treatment of Chronic Lymphocytic Leukemia (CLL)
Current Drug Delivery JAK2 as a Molecular Marker in Myeloproliferative Diseases
Cardiovascular & Hematological Agents in Medicinal Chemistry Insulin-Like Growth Factor 1 Receptor Targeted Therapeutics: Novel Compounds and Novel Treatment Strategies for Cancer Medicine
Recent Patents on Anti-Cancer Drug Discovery The Clinical and Immunological Features of Patients with Primary Antibody Deficiencies
Endocrine, Metabolic & Immune Disorders - Drug Targets Stem Cells in Amyotrophic Lateral Sclerosis: Motor Neuron Protection or Replacement?
CNS & Neurological Disorders - Drug Targets An Update on the Systemic Therapy of Malignant Salivary Gland Cancers: Role of Chemotherapy and Molecular Targeted Agents
Current Medicinal Chemistry - Anti-Cancer Agents