基本説明
Demonstrates how to apply the whole range of bioinformatics, chemoinformatics and molecular modeling tools to the rational design of novel drugs targeting GPCRs.
Full Description
G protein-coupled receptors (GPCRs) are one of the most important target classes in pharmacology and are the target of many blockbuster drugs. Yet only with the recent elucidation of the rhodopsin structure have these receptors become amenable to a rational drug design. Based on recent examples from academia and the pharmaceutical industry, this book demonstrates how to apply the whole range of bioinformatics, chemoinformatics and molecular modeling tools to the rational design of novel drugs targeting GPCRs. This book is an essential reading for medicinal chemists and drug designers working with this largest class of drug targets in the human genome.
Contents
Preface. 1. G Protein-coupled Receptors in the Human Genome (R. Fredriksson & H. Schioth). 2. Why G Protein-coupled Receptors Databases are Needed (J. Haiech, et al.). 3. A Novel Drug Screening Assay for G Protein-coupled Receptors (B. O'Dowd, et al.). 4. Importance of GPCR Dimerization for Function: The Case of the Class C GPCRs (L. Prezeau, et al.). 5. Molecular Mechanisms of GPCR Activation (R. Bywater & P. Denny-Gouldson). 6. Allosteric Properties and Regulation of G Protein-coupled Receptors (J. Galzi, et al.). 7. Chemogenomics Approaches to Ligand Design (T. Klabunde). 8. Strategies for the Design of pGPCR-targeted Libraries (N. Savchuk, et al.). 9. Ligand-based Rational Design: Virtual Screening (D. Clark & C. Higgs). 10. 3-D Structure of G Protein-coupled Receptors (L. Pardo, et al.). 11. 7TM Models in Structure-based Drug Design (F. Blaney, et al.). 12. Receptor-based Rational Design: Virtual Screening (D. Rognan). Subject Index.
