EPIGENETICS FOR DRUG DISCOVERY

Product description Review Select Guide Rating From the Inside Flap Epigenetics is one of the fastest moving fields in drug discovery, with almost every large pharmaceutical company and a substantial number of biotechnology companies targeting epigenetic processes to treat diseases ranging from cancer to Huntington s disease and from inflammation to sickle cell anaemia. The book will be structured in three main sections. The first section will introduce epigenetics and explain its importance at both a phenomenological and molecular level. The second section will go on to review how each of the big breakthroughs in drug discovery in this field have developed, with a strong emphasis on case histories. The final section will highlight the ongoing challenges in creating safe and efficacious epigenetic drugs.Written and edited by experts within the field from both industry and academia, this book will provide an invaluable guide to this developing field for medicinal chemists working in academia and in the pharmaceutical industry. From the Back Cover Epigenetics is one of the fastest moving fields in drug discovery, with almost every large pharmaceutical company and a substantial number of biotechnology companies targeting epigenetic processes to treat diseases ranging from cancer to Huntington’s disease and from inflammation to sickle cell anaemia. The book will be structured in three main sections. The first section will introduce epigenetics and explain its importance at both a phenomenological and molecular level. The second section will go on to review how each of the big breakthroughs in drug discovery in this field have developed, with a strong emphasis on case histories. The final section will highlight the ongoing challenges in creating safe and efficacious epigenetic drugs.Written and edited by experts within the field from both industry and academia, this book will provide an invaluable guide to this developing field for medicinal chemists working in academia and in the pharmaceutical industry. Excerpt. © Reprinted by permission. All rights reserved. Epigenetics for Drug DiscoveryBy Nessa CareyThe Royal Society of ChemistryCopyright © 2016 The Royal Society of ChemistryAll rights reserved.ISBN: 978-1-84973-882-8ContentsChapter 1 Epigenetics – What it is and Why it Matters Karl P. Nightingale, 1, Chapter 2 Enzyme and Protein Families that Regulate Histone Modifications and Crosstalk Charlotte E. Rutledge and Bryan M. Turner, 20, Chapter 3 Epigenetics and Disease Adele Murrell, 47, Chapter 4 Targeting DNA Methylation Tom D. Heightman and Michael McCullar, 68, Chapter 5 Targeting Histone Acetylation Daniel Vitt, Roland Baumgartner, and Hella Kohlhof, 96, Chapter 6 Targeting Histone Lysine Methyltransferases in Cancer Patrick Trojer, 127, Chapter 7 Targeting Non-Acetylation Histone Erasers Fei Lu and Hui Zhang, 168, Chapter 8 Progress in Targeting Epigenetic Readers Chun-wa Chung, 192, Chapter 9 Who will Benefit from Epigenetic Drugs? Dominique Verhelle and David J. Shields, 230, Chapter 10 Dosing – When Less is More Kurinji Pandiyan, Peter A. Jones, and Stephen B. Baylin, 249, Chapter 11 Histone Methyltransferase Activity Assays Haiching Ma, Konrad T. Howitz, Kurumi Y. Horiuchi, and Yuren Wang, 267, Chapter 12 Safety Considerations for Epigenetic Mechanisms as Drug Targets: Are Existing Toxicology Studies Fit for Purpose? Paul Butler, Michael Lawton, Robert E. Chapin, Brett D. Hollingshead, Karen Leach, Prashant R. Nambiar, Mathew Pletcher, and Amy H. Yang, 288, Subject Index, 316, CHAPTER 1Epigenetics – What it is and Why it MattersKARL P. NIGHTINGALE1.1 IntroductionThe last few years have witnessed explosive growth in the broad field of epigenetics, with the emergence of new paradigms, and the discovery of novel regulatory processes and molecules. This offers new approaches to understanding fundamental biology, but also promises new insight into disease processes, and the potential to modulate the genes involved.What then are epigenetic phenomena? In the broadest sense 'epigenetics' describes a layer of information and processes, which act in combination with the DNA sequence to determine an organism's characteristics (i.e. the 'phenotype' – hair colour, height, etc.). This concept is encompassed in the word epigenetics itself, where the Greek prefix 'epi-' suggests these are processes that are 'on top of' or 'in addition to' genetic effects. As such, genetic effects describe a change in gene activity and phenotype, due to a change in the DNA sequence (i.e. when genes are rearranged or mutated). In contrast, an epigenetic change is where gene expression and the phenotype are altered, but without a change in the DNA sequence – although there may be a change in the DNA's chemical modification or its packaging within the nucleus.There are three reasons for the intense interest in this field: (i) epigenetic mechanisms are involved in many fundamental areas of biology, and are often underpinned by novel, in