Abstract
Epigenetics is defined as heritable changes in gene expresssion, i.e. the presentation of a certain phenotype, without alterations to the genetic code. This is a central phenomenon in developmental biology but also for the pathogenesis of a variety of diseases, e.g. for cancer in the case of silencing of tumor suppressor proteins. Reversible histone acetylation is an important player within the epigenetic machinery and histone deacetylases are the best studied epigenetic target for drug discovery. A first drug (vorinostat) is already approved for human cancer treatment. The strategies and protocols for monitoring histone deacetylase (HDAC) activity are an integral part of drug discovery approaches towards new HDAC inhibitors and will be reviewed in this article. The main focus is on biochemical in-vitro assays but cellular hit validation models are also presented.
Current Topics in Medicinal Chemistry
Title: Assays for Histone Deacetylases
Volume: 9 Issue: 3
Author(s): Alexander-Thomas Hauser, Mira Jung and Manfred Jung
Affiliation:
Abstract: Epigenetics is defined as heritable changes in gene expresssion, i.e. the presentation of a certain phenotype, without alterations to the genetic code. This is a central phenomenon in developmental biology but also for the pathogenesis of a variety of diseases, e.g. for cancer in the case of silencing of tumor suppressor proteins. Reversible histone acetylation is an important player within the epigenetic machinery and histone deacetylases are the best studied epigenetic target for drug discovery. A first drug (vorinostat) is already approved for human cancer treatment. The strategies and protocols for monitoring histone deacetylase (HDAC) activity are an integral part of drug discovery approaches towards new HDAC inhibitors and will be reviewed in this article. The main focus is on biochemical in-vitro assays but cellular hit validation models are also presented.
Export Options
About this article
Cite this article as:
Hauser Alexander-Thomas, Jung Mira and Jung Manfred, Assays for Histone Deacetylases, Current Topics in Medicinal Chemistry 2009; 9 (3) . https://dx.doi.org/10.2174/156802609788085269
DOI https://dx.doi.org/10.2174/156802609788085269 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
- Announcements
Related Articles
-
Dendrimers - Nanoparticles with Precisely Engineered Surfaces
Current Organic Chemistry Interaction of Macrocyclic Lactones with the Multidrug Transporters: The Bases of the Pharmacokinetics of Lipid-Like Drugs
Current Drug Metabolism Innovative Stride to Zero Hunger Beyond 2015 in Nigeria
Recent Patents on Food, Nutrition & Agriculture Preparation, Characterization, and In Vitro Release of Vinorelbine Tartrate (VLBT)- Loaded Folate-conjugated Recombination Human Serum Albumin (rHSA) Nanoparticles with Different Degree of Cross-linking
Current Nanoscience State of the Art of the Bi- and Trimetallic Nanoparticles on the Basis of Gold and Iron
Recent Patents on Nanotechnology Chemistry of Plant Dyes: Applications and Environmental Implications of Dyeing Processes
Current Environmental Engineering Evaluation of the Soluble Pectin Content in Culinary Preparations
Current Nutrition & Food Science Diterpenoids from Liverworts and their Biological Activities
Current Organic Chemistry Conventional and Novel Approaches in Generating and Characterization of Reactive Intermediates from Drugs/Drug Candidates
Current Drug Metabolism Non-allowed Pharmacologically Active Substances in Physical and Sexual Performance Enhancing Products
Current Neuropharmacology A Novel Method for the Analysis of Soluble Carbohydrates from Cistanche deserticola
Current Analytical Chemistry Evaluation of the Food and Nutrition Value of Rubus alceifolius Poir. Fruits of Mizoram, India
Current Nutrition & Food Science Biological Activities of Eco-Friendly Synthesized Hantzsch Adducts
Medicinal Chemistry Evaluation on Monocyte-Mediated Delivery of a Therapeutic Gene into the Inflamed Brain
Current Gene Therapy Potential of Nanocarriers in Genetic Immunization
Recent Patents on Drug Delivery & Formulation The Effect of Educational Intervention Based on Health Belief Model on Beliefs Towards Human Papillomavirus Vaccination in a Sample of Iranian Female Nursing Students
Current Women`s Health Reviews Strategies of Functional Foods Promote Sleep in Human Being
Current Signal Transduction Therapy Development of Functional Dark Chocolate by Incorporating Flaxseed (Linum usitatissimum) Oil and Honey with Improved Organoleptic and Textural Attributes
Current Nutrition & Food Science Nanotechnology approaches for pain therapy through transdermal drug delivery
Current Pharmaceutical Design Alternative Gene Therapy Strategies for the Repair of Craniofacial Bone Defects
Current Gene Therapy