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Epigenetic Drug Discovery /
| Clasificación: | Libro Electrónico |
|---|---|
| Otros Autores: | , |
| Formato: | Electrónico eBook |
| Idioma: | Inglés |
| Publicado: |
Weinhem, Germany :
Wiley-VCH,
2018.
©2019 |
| Colección: | Methods and Principles in Medicinal Chemistry Ser.
|
| Temas: | |
| Acceso en línea: | Texto completo |
Tabla de Contenidos:
- Cover; Title Page; Copyright; Preface; Foreword; Contents; Part I Introduction
- Epigenetics; Chapter 1 Epigenetics: Moving Forward; 1.1 Why This Enormously Increased Interest?; 1.2 Looking Forward to New Avenues of Epigenetics; Acknowledgments; References; Part II General Aspects/Methodologies; Chapter 2 Structural Biology of Epigenetic Targets: Exploiting Complexity; 2.1 Introduction; 2.2 DNA Methylases: The DNMT3A-DNMT3L-H3 and DNMT1-USP7 Complexes; 2.3 Histone Arginine Methyltransferases: The PRMT5-MEP50 Complex
- 2.4 Histone Lysine Methyltransferases: The MLL3-RBBP5-ASH2L and the PRC2 Complexes2.5 Histone Lysine Ubiquitinylases: The PRC1 Complex; 2.6 Histone Lysine Deubiquitinylases: The SAGA Deubiquitination Module; 2.7 Histone Acetyltransferases: The MSL1 and NUA4 Complexes; 2.8 Histone Deacetylases: HDAC1-MTA1 and HDAC3-SMRT Complexes and HDAC6; 2.9 Histone Variants and Histone Chaperones: A Complex and Modular Interplay; 2.10 ATP-Dependent Remodelers: CHD1, ISWI, SNF2, and the SNF2-Nucleosome Complex
- 2.11 Epigenetic Readers: Histone Crotonylation Readers and the 53BP1-Nucleosome (H2AK15Ub-H4K20me2) Complex2.12 Conclusions; Acknowledgments; References; Chapter 3 Computer-based Lead Identification for Epigenetic Targets; 3.1 Introduction; 3.2 Computer-based Methods in Drug Discovery; 3.2.1 Pharmacophore-based Methods; 3.2.2 QSAR; 3.2.3 Docking; 3.2.4 Virtual Screening; 3.2.5 Binding Free Energy Calculation; 3.3 Histone Deacetylases; 3.3.1 Zinc-Dependent HDACs; 3.3.2 Sirtuins; 3.4 Histone Methyltransferases; 3.5 Histone Demethylases; 3.5.1 LSD1 (KDM1A); 3.5.2 Jumonji Histone Demethylases
- 3.6 SummaryAcknowledgments; References; Chapter 4 Mass Spectrometry and Chemical Biology in Epigenetics Drug Discovery; 4.1 Introduction: Mass Spectrometry Technology Used in Epigenetic Drug Discovery; 4.1.1 Mass Spectrometry Workflows for the Analysis of Proteins; 4.1.2 Mass Spectrometry Imaging; 4.2 Target Identification and Selectivity Profiling: Chemoproteomics; 4.2.1 Histone Deacetylase and Acetyltransferase Chemoproteomics; 4.2.2 Bromodomain Chemoproteomics; 4.2.3 Demethylase Chemoproteomics; 4.2.4 Methyltransferase Chemoproteomics
- 4.3 Characterization of Epigenetic Drug Target Complexes and Reader Complexes Contributing to Drug's Mode of Action4.3.1 Immunoaffinity Purification of Native Protein Complexes; 4.3.2 Immunoaffinity Purification with Antibodies Against Epitope Tags; 4.3.3 Affinity Enrichment Using Histone Tail Peptides as Bait; 4.4 Elucidation of a Drug's Mode of Action: Analysis of Histone Posttranslational Modifications by MS-Based Proteomics; 4.4.1 Histone Modification MS Workflows; 4.4.2 Application of Histone MS Workflows to Characterize Epigenetic Drugs; 4.5 Challenges and New Trends