Epigenetic Targets In Drug Discovery

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Epigenetic Targets In Drug Discovery

Author : Wolfgang Sippl
ISBN : 3527323554
Genre : Medical
File Size : 26.92 MB
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Fueled by the expertise of a team of international specialist authors, this first reference on the booming topic covers everything a drug researcher needs to know about targeting epigenetic mechanisms of disease. The first part of the book surveys current methodologies for finding and validating drug candidates that act via epigenetic mechanisms. The second part systematically surveys known and suspected drug targets within the epigenetic machinery, including the discovery and development of vorinostat, the first marketed epigenetic drug.
Category: Medical

Epigenetic Drug Discovery

Author : Wolfgang Sippl
ISBN : 9783527343140
Genre : Medical
File Size : 58.72 MB
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This broad view of epigenetic approaches in drug discovery combines methods and strategies with individual targets, including new and largely unexplored ones such as sirtuins and methyl-lysine reader proteins. Presented in three parts - Introduction to Epigenetics, General Aspects and Methodologies, and Epigenetic Target Classes - it covers everything any drug researcher would need in order to know about targeting epigenetic mechanisms of disease. Epigenetic Drug Discovery is an important resource for medicinal chemists, pharmaceutical researchers, biochemists, molecular biologists, and molecular geneticists.
Category: Medical

Epigenetics For Drug Discovery

Author : Nessa Carey
ISBN : 9781849738828
Genre : Science
File Size : 29.58 MB
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This book will provide an invaluable guide to epigenetics, one of the fastest moving fields in drug discovery, for medicinal chemists working in academia and in the pharmaceutical industry.
Category: Science

Epi Informatics

Author : Jose Medina-Franco
ISBN : 9780128028094
Genre : Medical
File Size : 33.79 MB
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Epi-Informatics: Discovery and Development of Small Molecule Epigenetic Drugs and Probes features multidisciplinary strategies with strong computational approaches that have led to the successful discovery and/or optimization of compounds that act as modulators of epigenetic targets. This book is intended for all those using or wanting to learn more about computational methodologies in epigenetic drug discovery, including molecular modelers, informaticians, pharmaceutical scientists, and medicinal chemists. With a better understanding of different molecular modeling and cheminformatic approaches, readers can incorporate these techniques into their own drug discovery projects that may involve chemical synthesis and medium- or high-throughput screening. In addition, this book highlights the significance of epigenetic targets to the public health for molecular modelers and chemoinformatians. The goal of this reference is to stimulate ongoing multidisciplinary research and to further improve current computational methodologies and workflows in order to accelerate the discovery and development of epi-drugs and epi-probes. Focuses on the discovery of epi-drugs as candidates to be used in therapy including combined therapies Describes new computational methodologies and screening assays utilizing recent and emerging novel structural data Highlights the discovery, development and optimization of epi-probes, which are molecular probes that elucidate epigenetic mechanisms Includes important topics such as computational-guided optimization of epi-hits, virtual screening to identify novel compounds for epigenetic targets, development and mining of epigenetic molecular databases, SAR modeling of screening data and much more
Category: Medical

Drug Discovery In Cancer Epigenetics

Author : Gerda Egger
ISBN : 9780128024928
Genre : Medical
File Size : 67.19 MB
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Drug Discovery in Cancer Epigenetics is a practical resource for scientists involved in the discovery, testing, and development of epigenetic cancer drugs. Epigenetic modifications can have significant implications for translational science as biomarkers for diagnosis, prognosis or therapy prediction. Most importantly, epigenetic modifications are reversible and epigenetic players are found mutated in different cancers; therefore, they provide attractive therapeutic targets. There has been great interest in developing and testing epigenetic drugs, which inhibit DNA methyltransferases, histone modifying enzymes or chromatin reader proteins. The first few drugs are already FDA approved and have made their way into clinical settings. This book provides a comprehensive summary of the epigenetic drugs currently available and aims to increase awareness in this area to foster more rapid translation of epigenetic drugs into the clinic. Highlights the potential of epigenetic alterations in cancer for drug development Covers the tools and methods for epigenetic drug discovery, preclinical and clinical testing, and clinical implications of epigenetic therapy Provides important information regarding putative epigenetic targets, epigenetic technologies, networks and consortia for epigenetic drug discovery and routes for translation
Category: Medical

Gynecological Cancers

Author : Antonio Giordano
ISBN : 9783319329079
Genre : Medical
File Size : 87.29 MB
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Facilitating the collaboration between the basic, translational, and clinical sciences, this book provides an overview of the genetic and epigenetic mechanisms underlying the formation and progression of gynecological cancers. Gynecological Cancers: Genetic and Epigenetic Targets and Drug Development gathers all of the molecular and cellular aspects of gynecological cancer together within one volume, providing detailed and up-to-date information on the etiology, diagnosis, and treatment of gynecological cancers. Gynecological Cancers: Genetic and Epigenetic Targets and Drug Development ​also discusses the racial and ethnic disparities in the treatment of gynecological cancers through cost effective modalities like single visit screening and diagnosis, well women clinics, and mobile clinics. Written and edited by leaders in the field, this volume within the Current Clinical Oncology series is an indispensable resource for today’s practicing oncologist.
Category: Medical

Epigenetic Approaches In Drug Discovery Development And Treatment

Author : Shibashish Giri
ISBN : 9782889639328
Genre :
File Size : 42.26 MB
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Establishment of a normal phenotype involves dynamic epigenetic regulation of gene expression that when affected contributes to human diseases. On a molecular level, epigenetic regulation is marked by specific covalent modifications (acetylation, methylation, phosphorylation, sumoylation, PARylation and ubiquitylation) of DNA and its associated histones. Studies also suggest the influence of such epigenetic modifications on non-coding RNA expression implicated in normal and diseased phenotypes. Epigenetic control of genetic expression is a reversible process essential for normal development and function of an organism. Alteration of epigenetic regulation leads to various disease forms such as cancer, diabetes, inflammation and neuropsychiatric disorders. Assessing these alterations provides a deeper insight into the changes induced in the genome, which is often informative for identifying disease subtypes or developing suitable treatments. Therefore, epigenetics proves to be a key area of clinical investigation in diagnosis, prognosis, and treatment of complex diseases. Genetic mutations, environmental stress, pathogens and drugs of abuse are some of the predominant factors that induce and impact changes on chromatin, which directly dictate a diseased phenotype. It is essential to consider the interaction between genetic and epigenetic factors to understand the molecular mechanisms of complex human diseases for safer and efficient drug development. Furthermore, genetic variation in absorption, distribution, metabolism, and excretion (ADME) genes is insufficient to account for interindividual variability of drug response. Therefore, current efforts aim to identify epigenetic components of ADME gene regulation, which include phase-I and phase-II enzymes, uptake transporters, efflux transporters and nuclear receptors involved in regulation of ADME genes. Monitoring circulatory epigenetic biomarkers in liquid biopsies (blood, saliva, urine, cerebrospinal fluid) of disease-associated and drug-associated epigenetic alterations may prove useful for decision support for routine clinical treatment and drug discovery. Hence, recent drug discovery efforts on targeting the epigenome, has emerged an area of interest with several new drugs being developed, tested and some already approved by the US Food and Drug Administration (FDA). These new insights into the complexities of epigenetic regulation are key contributors to our basic understanding of this process in human health and disease, which will provide scope for innovative drug therapies. It is of urgency to aid the present understanding of epigenomics driven diseased outcomes, with the expectation that further studies will identify early markers of disease and targets for therapeutics.
Category:

Gynecological Cancers

Author : Antonio Giordano
ISBN : 3319329057
Genre : Medical
File Size : 55.25 MB
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Facilitating the collaboration between the basic, translational, and clinical sciences, this book provides an overview of the genetic and epigenetic mechanisms underlying the formation and progression of gynecological cancers. Gynecological Cancers: Genetic and Epigenetic Targets and Drug Development gathers all of the molecular and cellular aspects of gynecological cancer together within one volume, providing detailed and up-to-date information on the etiology, diagnosis, and treatment of gynecological cancers. Gynecological Cancers: Genetic and Epigenetic Targets and Drug Development ​also discusses the racial and ethnic disparities in the treatment of gynecological cancers through cost effective modalities like single visit screening and diagnosis, well women clinics, and mobile clinics. Written and edited by leaders in the field, this volume within the Current Clinical Oncology series is an indispensable resource for today’s practicing oncologist.
Category: Medical

Epigenetics In Psychiatry

Author : Jacob Peedicayil
ISBN : 9780124171343
Genre : Science
File Size : 73.31 MB
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Epigenetics in Psychiatry covers all major areas of psychiatry in which extensive epigenetic research has been performed, fully encompassing a diverse and maturing field, including drug addiction, bipolar disorder, epidemiology, cognitive disorders, and the uses of putative epigenetic-based psychotropic drugs. Uniquely, each chapter correlates epigenetics with relevant advances across genomics, transcriptomics, and proteomics. The book acts as a catalyst for further research in this potentially very important and useful area of psychiatry. The elucidation of basic principles of epigenetic biology points to the creation of more optimal and effective therapies for major classes of psychiatric disease. In this regard, epigenetic therapy, the use of drugs to correct epigenetic defects, may help in the pharmacotherapy of patients with these disorders. With time, such advances may eventually point to replacements for psychotropic drugs presently of symptomatic value and low efficacy. Moreover, there is evidence to suggest that other forms of treatment commonly used in the management of psychiatric disorders, like psychotherapy and electroconvulsive therapy, may also act by epigenetic mechanisms. Chapters review fascinating new areas of research across neuronal stem cells, cognitive disorders, and transgenerational epigenetics through drug addiction Relates broad advances in psychiatric epigenetics to a modern understanding of the genome, transcriptome, and protein Catalyzes knowledge discovery in both basic epigenetic biology and clinical application as epigenetic targets for drug discovery
Category: Science

Clinical And Statistical Considerations In Personalized Medicine

Author : Claudio Carini
ISBN : 9781466593879
Genre : Mathematics
File Size : 26.80 MB
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The Future of Clinical Research and Health Care: From Empirical to Precision Medicine Clinical and Statistical Considerations in Personalized Medicine explores recent advances related to biomarkers and their translation into clinical development. Leading clinicians, biostatisticians, regulators, commercial professionals, and researchers address the opportunities and challenges in successfully applying biomarkers in drug discovery and preclinical and clinical development. Robust Biomarkers for Drug Development and Disease Treatment The first four chapters discuss biomarker development from a clinical perspective. Coverage ranges from an introduction to biomarkers to advances in RNAi screens, epigenetics, and rare diseases as targets for personalized medicine approaches. Subsequent chapters examine the statistical considerations in applying a personalized medicine approach, including multiplicity in pharmacogenomics. The last chapter assesses the regulatory issues involved in using biomarkers. Improve Patient Care and Reduce Costs and Side Effects Despite the vast amount of literature on biomarkers, there is no comprehensive book that integrates the clinical and statistical components. This book is one of the first to incorporate both the clinical and statistical aspects of biomarkers in the personalized medicine paradigm. Covering a wide spectrum of personalized medicine-related topics, it presents state-of-the-art techniques for advancing the application of biomarkers in drug discovery and development.
Category: Mathematics

Multifaceted Roles Of Crystallography In Modern Drug Discovery

Author : Giovanna Scapin
ISBN : 9789401797191
Genre : Science
File Size : 90.71 MB
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The present work offers a snapshot of the state-of-the-art of crystallographic, analytical, and computational methods used in modern drug design and development. Topics discussed include: drug design against complex systems (membrane proteins, cell surface receptors, epigenetic targets, and ribosomes); modulation of protein-protein interactions; the impact of small molecule structures in drug discovery and the application of concepts such as molecular geometry, conformation, and flexibility to drug design; methodologies for understanding and characterizing protein states and protein-ligand interactions during the drug design process; and monoclonal antibody therapies. These methods are illustrated through their application to problems of medical and biological significance, such as viral and bacterial infections, diabetes, autoimmune disease, and CNS diseases. As approaches to drug discovery have changed over time, so have the methodologies used to solve the varied, new, and difficult problems encountered in drug discovery. In recent years we have seen great progress in the fields of genetics, biology, chemistry, and medicine, but there are still many unmet medical needs, from bacterial infections to cancer to chronic maladies, that require novel, different, or better therapies. This work will be of interest to researchers and policy makers interested in the latest developments in drug design.
Category: Science

Chemical Epigenetics

Author : Antonello Mai
ISBN : 9783030429829
Genre : Science
File Size : 38.43 MB
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This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.
Category: Science

Comprehensive Analysis Of Parasite Biology

Author : Sylke M?ller
ISBN : 9783527339044
Genre : Medical
File Size : 66.89 MB
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Written and edited by experts in the field, this book brings together the current state of the art in phenotypic and rational, target-based approaches to drug discovery against pathogenic protozoa. The chapters focus particularly on virtual compounds and high throughput screening, natural products, computer-assisted drug design, structure-based drug design, mechanism of action identification, and pathway modelling. Furthermore, state-of the art "omics" technologies are described and currently studied enzymatic drug targets are discussed. Mathematical, systems biology-based approaches are introduced as new methodologies for dissecting complex aspects of pathogen survival mechanisms and for target identification. In addition, recently developed anti-parasitic agents targeting particular pathways, which serve as lead compounds for further drug development, are presented.
Category: Medical

Fragment Based Drug Discovery

Author : Daniel A. Erlanson
ISBN : 9783527337750
Genre : Medical
File Size : 80.46 MB
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From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets.
Category: Medical

Protein Interactions As Targets In Drug Discovery

Author : Rossen Donev
ISBN : 9780128168462
Genre :
File Size : 27.50 MB
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Protein Interactions as Targets in Drug Discovery, Volume 121, is dedicated to the design of therapeutics, both experimental and computational, that target protein interactions. Chapters in this new release include Trends in structure based drug design with protein targets, From fragment- to peptide-protein interaction: addressing the structural basis of binding using Supervised Molecular Dynamics (SuMD), Protein-protein and protein-ligand interactions: identification of potential inhibitors through computational analysis, Aromatic-aromatic interactions in protein-drug and protein-protein interactions, Role of protein-protein interaction in allosteric drug design within the human methyltransferome, and much more.
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Pharmacoepigenetics

Author :
ISBN : 9780128139400
Genre : Medical
File Size : 61.3 MB
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Pharmacoepigenetics, Volume Eleven provides a comprehensive volume on the role of epigenetics and epigenomics in drug discovery and development, providing a detailed, but accessible, view of the field, from basic principles, to applications in disease therapeutics. Leading international researchers from across academia, clinical settings and the pharmaceutical industry discuss the influence of epigenetics and epigenomics in human pathology, epigenetic biomarkers for disease prediction, diagnosis, and treatment, current epigenetic drugs, and the application of epigenetic procedures in drug development. Throughout the book, chapter authors offer a balanced and objective discussion of the future of pharmacoepigenetics and its crucial contribution to the growth of precision and personalized medicine. Fully examines the influence of epigenetics and epigenomics in human pathology, epigenetic biomarkers for disease prediction, diagnosis, treatment, current epigenetic drugs and the application of epigenetic procedures in drug development Features chapter contributions from leading international researchers in academia, clinical settings and the pharmaceutical industry Instructs researchers, students and clinicians on how to better interpret and employ pharmacoepigenetics in drug development, efficiency and safety Provides a balanced and objective discussion of the future of pharmacoepigenetics and its crucial role in precision medicine
Category: Medical

Epigenetic Therapy Of Cancer

Author : Michael Lübbert
ISBN : 9783642384042
Genre : Medical
File Size : 51.15 MB
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The growing knowledge about disturbances of epigenetic gene regulation in hematopoietic stem cell disorders is now being translated into treatment approaches that target the epigenetic defects pharmacologically. This book first presents the latest evidence regarding the epigenetic regulation of hematopoietic stem cell differentiation and hemoglobin production. The significance of DNA methylation abnormalities in hematopoietic disorders and of epigenetic disturbances in lung cancer and other solid tumors is then discussed. A major part of the book, however, relates specifically to the translation of basic research and drug development to clinical applications, and in this context both present and future clinical strategies are considered. Individual chapters are devoted to the use of DNA hypomethylating agents and chromatin-modifying agents, and the treatment of hematologic malignancies and solid tumors by means of epigenetic agents is discussed in detail.
Category: Medical

Therapeutic Targets

Author : Luis M. Botana
ISBN : 9781118185520
Genre : Medical
File Size : 71.59 MB
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The Latest Applications For Cellmechanism Research in Drug Discovery Designed to connect research on cell mechanisms with the drug discovery process, Therapeutic Targets: Modulation, Inhibition, and Activation introduces readers to a range of new concepts and novel approaches to drug screening and therapeutic drug targeting to help inform future avenues of drug research. Highly topical, this accessible edited volume features chapters contributed by respected experts from around the globe. The book helps postgraduate students and professional scientists working in academia and industry understand the molecular mechanisms of pharmacology, current pharmacological knowledge, and future perspectives in drug discovery, focusing on important biochemical protein targets and drug targeting strategies for specific diseases. Examining the pharmacology of therapeutically undefined targets and their potential applications, it includes chapters on traditional therapeutic targets, including enzymes (phosphodiesterases and proteases), ion channels, and G protein-coupled receptors, as well as more recently identified avenues of exploration, such as lipids, nuclear receptors, gene promoters, and more. Since different diseases require different targeting techniques, the book also includes dedicated chapters on strategies for investigating Alzheimer's, diabetes, pain, and inflammation treatments. Concluding with a cross-sectional look at new approaches in drug screening, Therapeutic Targets is an invaluable resource for understanding where the next generation of drugs are likely to emerge.
Category: Medical

Epigenetics In Cardiovascular Disease

Author : Yvan Devaux
ISBN : 9780128222591
Genre : Medical
File Size : 37.45 MB
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Epigenetics in Cardiovascular Disease, a new volume in the Translational Epigenetics series, offers a comprehensive overview of the epigenetics mechanisms governing cardiovascular disease development, as well as instructions in research methods and guidance in pursing new studies. More than thirty international experts provide an (i) overview of the epigenetics mechanisms and their contribution to cardiovascular disease development, (i) high-throughput methods for RNA profiling including single-cell RNA-seq, (iii) the role of nucleic acid methylation in cardiovascular disease development, (iv) epigenetic actors as biomarkers and drug targets, (v) and the potential of epigenetics to advance personalized medicine. Here, readers will discover strategies to combat research challenges, improve quality of their epigenetic research and reproducibility of their findings. Additionally, discussion of assay and drug development for personalized healthcare pave the way for a new era of understanding in cardiovascular disease. Offers a thorough overview of role of epigenetics mechanisms in cardiovascular disease Includes guidance to improve research plans, experimental protocols design, quality and reproducibility of results in new epigenetics research Explores biomarkers and drug targets of therapeutic potential to advance personalized healthcare Features chapter contributions from a wide range of international researchers in the field
Category: Medical

Dna And Histone Methylation As Cancer Targets

Author : Atsushi Kaneda
ISBN : 9783319597867
Genre : Medical
File Size : 39.75 MB
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This book will focus on DNA and histone methylation in epigenetics and describe how it is involved in the molecular mechanisms responsible for the development of cancer. Chapters will summarize the current knowledge of the molecular basis of DNA and histone methylation and explain how it is involved in cancer, describe the features of DNA and histone methylation associated with particular types of cancer, diagnostic/therapeutic applications, and future directions of DNA and histone methylation as cancer targets.
Category: Medical