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Recent advances in class IIa histone deacetylases research
Affiliation:1. School of Pharmacy, College of Pharmacy, Taipei Medical University, 250 Wuxing Street, Taipei, 11031, Taiwan;2. Ph.D. Program for Clinical Drug Development of Chinese Herbal Medicine, College of Pharmacy, Taipei Medical University, Taiwan;3. TMU Biomedical Commercialization Center, Taipei Medical University, Taiwan;4. The Ph.D. Program for Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan;5. Division of Hematology/Oncology, Department of Internal Medicine, National Cheng King University Hospital, College of Medicine, National Cheng King University, Tainan, Taiwan;6. National Institute of Cancer Research, National Health Research Institutes, Tainan, 704, Taiwan;1. Institute of Pharmaceutical and Medicinal Chemistry, Heinrich-Heine-University Düsseldorf, 40225 Düsseldorf, Germany;1. Department of Pharmaceutical Chemistry, JSS College of Pharmacy (A Constituent College of JSS University, Mysuru), Ootacamund 643 001, Tamil Nadu, India;2. TIFAC CORE, JSS College of Pharmacy (A Constituent College of JSS University, Mysuru), Ootacamund, Tamil Nadu, India;1. Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran;2. Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran;1. Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, Shanghai, 201203, China;2. School of Chemistry & Chemical Engineering, Shanghai University of Engineering Science, Shanghai, 201620, China;3. School of Pharmacy, Fudan University, Shanghai, 201203, China;1. Institute for Molecular Bioscience (IMB), The University of Queensland, Brisbane, Queensland 4072, Australia;2. IMB Centre for Inflammation and Disease Research and Australian Infectious Diseases Research Centre, The University of Queensland, Brisbane, Queensland 4072, Australia;3. ARC Centre of Excellence in Advanced Molecular Imaging, IMB, The University of Queensland, Brisbane, Queensland 4072, Australia;4. School of Pharmacy, The University of Queensland, Brisbane, Queensland 4072, Australia;5. Metabolomics Australia, Australian Institute for Bioengineering and Nanotechnology, The University of Queensland, Brisbane, Queensland 4072, Australia;6. Victor Chang Cardiac Research Institute, Sydney, New South Wales 2010, Australia;7. CSIRO-QUT Synthetic Biology Alliance, Centre for Tropical Crops and Biocommodities, Queensland University of Technology (QUT), Gardens Point Campus, Brisbane, Queensland 4000, Australia;8. The University of Queensland Diamantina Institute, The University of Queensland, Brisbane, Queensland 4072, Australia;9. Australian Prostate Cancer Research Centre-Queensland, Institute of Health and Biomedical Innovation, School of Biomedical Sciences, Faculty of Health, Translational Research Institute, Queensland University of Technology (QUT), Brisbane, Queensland 4102, Australia
Abstract:Epigenetic control plays an important role in gene regulation through chemical modifications of DNA and post-translational modifications of histones. An essential post-translational modification is the histone acetylation/deacetylation-process which is regulated by histone acetyltransferases (HATs) and histone deacetylases (HDACs). The mammalian zinc dependent HDAC family is subdivided into three classes: class I (HDACs 1-3, 8), class II (IIa: HDACs 4, 5, 7, 9; IIb: HDACs 6, 10) and class IV (HDAC 11). In this review, recent studies on the biological role and regulation of class IIa HDACs as well as their contribution in neurodegenerative diseases, immune disorders and cancer will be presented. Furthermore, the development, synthesis, and future perspectives of selective class IIa inhibitors will be highlighted.
Keywords:Histone deacetylases  Synthesis of HDACi  Anticancer activity  Neurodegenerative diseases  Immune disorders
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