Epigenetics for drug discovery / edited by Nessa Carey.

Format:

Book

Author/Creator:

Nessa Carey

Contributor:

Carey, Nessa, editor.

Royal Society of Chemistry (Great Britain), issuing body.

Series:

RSC drug discovery series ; Number 48.

RSC Drug Discovery Series, 2041-3203 ; Number 48

Language:

English

Subjects (All):

Pharmacogenetics.

Epigenetics.

Drug targeting.

Physical Description:

1 online resource (337 p.)

Place of Publication:

Cambridge, England : Royal Society of Chemistry, 2016.

Language Note:

English

Summary:

<P>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.</P>

Contents:

Cover; Epigenetics for Drug Discovery; Preface; Contents; Chapter 1 - Epigenetics - What it is and Why it Matters; 1.1 Introduction; 1.2 Beyond DNA: A Broad Picture of Epigenetic Mechanisms; 1.3 Gene Regulation and the Impact of Chromatin Assembly; 1.4 Chromatin Structure and the Basis of Epigenetic Mechanisms; 1.5 Gene Regulation in Chromatin: The Role of Epigenetic Mechanisms; 1.5.1 Chromatin Remodelling; 1.5.2 Histone Variants; 1.5.3 Histone Modification; 1.5.3.1 Drivers of Dynamic Gene Regulation: Histone-Modifying Enzymes; 1.5.4 DNA Methylation

1.6 Epigenetic Crosstalk - Integrating Histone Modification and DNA Methylation1.7 Summary; References; Chapter 2 - Enzyme and Protein Families that Regulate Histone Modifications and Crosstalk; 2.1 Histones: Endless Variations on a Highly Conserved Theme; 2.1.1 Organising DNA; 2.1.2 Histone Genes; 2.1.3 Post-Translational Modifications of Histones; 2.2 How Histone Modifications Influence Chromatin Function; 2.2.1 Associations between Modifications and Chromatin Function; 2.2.2 Nucleosome Signalling and the Histone Code Hypothesis

2.3 Enzymes that Write Histone Modifications and Protein Domains that Read them2.3.1 Histone Acetylation; 2.3.2 Histone Methylation; 2.3.3 The Multiple Readers of Histone Methylation; 2.3.4 Histone Phosphorylation; 2.4 Interactions between Histone Modifications - Crosstalk; 2.4.1 Effects on Further Modification of the Same Histone Tail; 2.4.2 Effects on Recognition of Nearby Modifications; 2.4.3 Effects on Erasure of Nearby Modifications; 2.5 The Importance of Protein Complexes; 2.5.1 HDACs and their Inhibitors; 2.6 Conclusions; Acknowledgements; References

Chapter 3 - Epigenetics and Disease3.1 Introduction; 3.2 Congenital Mendelian Inherited Epigenetic Diseases; 3.2.1 Mendelian Inherited Congenital Syndromes Involving Mutations in Genes that Encode DNA Methylation Readers and Modifiers; 3.2.1.1 Mutations in the DNMT Genes; 3.2.1.2 Mutations within DNA Methylation Readers; 3.3 Mendelian Inherited Congenital Syndromes Involving Mutations in Genes that Encode Histone Modifiers; 3.4 Mutations in Genes Encoding Nucleosomal Remodelling and Architectural Proteins; 3.5 Congenital NMEDs Exemplified by Syndromes Due to Loss of Genomic Imprinting

3.6 Complex Disease and Epigenetics3.7 Conclusions; References; Chapter 4 - Targeting DNA Methylation; 4.1 Introduction; 4.2 DNA Methylation and Its Role in Gene Expression; 4.3 Reversal and Modification of DNA Methylation; 4.4 Aberrant DNA Methylation in Cancer; 4.5 DNA Methylation in Other Diseases; 4.6 Structure and Mechanism of DNMTs; 4.7 DNMT Inhibitors; 4.7.1 Nucleoside DNMT Inhibitors; 4.7.2 Non-Nucleoside DNMT Inhibitors; 4.8 Outlook; Acknowledgements; References; Chapter 5 - Targeting Histone Acetylation; 5.1 Introduction; 5.2 HDAC Proteins; 5.2.1 Function of Histone Deacetylases

5.2.2 Regulation of Signalling Pathways and Phenotypes

Notes:

Description based upon print version of record.

Includes bibliographical references at the end of each chapters and index.

Description based on online resource; title from PDF title page (ebrary, viewed December 8, 2015).

ISBN:

9781782628484

1782628487