Areas covered: This article focuses on the concepts and drug discovery aspects of epigenomics. Ganesan A(1)(2). First, there are the so-called writers, enzymes that catalyse a structural modification of their protein or a nucleic acid macromolecular substrate. 213-357. •• This book chapter has discussed various chemoinformatic strategies for epigenetic drug discovery that can be utilized before designing and developing a screening library. Drug combination approaches also have included epigenetic targeting together with either conventional chemotherapy or selective therapies such as Gleevec. 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. Epigenetic regulation of gene expression can contribute to diseases such as cancer, inflammation and neuropsychiatric disorders. However, knowledge of the molecular mechanisms that underlie epigenetic regulation remains in its infancy, and is currently too limited to allow rapid development of molecular probes. 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 is structured in three main sections. Expert Opin Drug Discov, 9 (9) (2014), pp. Mohan CG (Ed.). CrossRef View Record in Scopus Google Scholar. Pharmacogenomics in Alzheimer’s disease. However, drug discovery has been slowed by a lack of a high-throughput screening method: Scientists currently visualize epigenetic changes using special dyes and traditional microscopy methods. This is Author information: (1)School of Pharmacy, University of East Anglia, Norwich NR4 7TJ, UK a.ganesan@uea.ac.uk. Epigenetic drug discovery for Alzheimer’s disease. Epigenetic enzymes have been important drug discovery and development targets for over a decade, but recent developments in epigenetic analysis technologies and methods, combined with increased investments from the major pharmaceutical companies are accelerating the use of this class of therapeutic drugs in the clinic. Wolfgang Sippl, PhD, holds the chair in Medicinal Chemistry at the Institute of Pharmacy at the Martin Luther University Halle-Wittenberg. In: Structural Bioinformatics: Applications in Preclinical Drug Discovery Process. Abstract:In recent years, there has been an expansion of the understanding of how epigenetic dysregulation plays a role in tumorigenesis, progression, metastasis and treatment resistance. Keywords:Epigenetic, anticancer drug discovery, DNA methylation, histone posttranslational modification. Epigenetic drug discovery: a success story for cofactor interference. Springer International Publishing, Cham, Switzerland, 247–269 (2019). Epigenetic research has progressed rapidly, and epigenetic processes are known to be crucial to the modulation of various diseases. R. Cacabelos. For convenience, epigenetic targets for drug discovery are grouped into three major families . (2)Freiburg Institute of Advanced Studies (FRIAS), University of Freiburg, 79104 Freiburg im Breisgau, Germany. About the Author. 1059-1086. Methods Mol Biol, 448 (2008), pp. Introduction: Epigenetic modification has been implicated in a wide range of diseases and the ability to modulate such systems is a lucrative therapeutic strategy in drug discovery. Epigenetic Drug Discovery is an important resource for medicinal chemists, pharmaceutical researchers, biochemists, molecular biologists, and molecular geneticists.
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