GPCRs: From Deorphanization to Lead Structure Identification
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Based on the international workshop GPCRs: From Deorphanisation to Lead StructureIdentification, held in Berlin in May 2006, the book highlights the following topics: Structure of GPCRs, Design of GPCR Ligands, GPCR Signalling, Deorphanization and Assay Development. All chapters are written by leading experts in the field, discussing the most recent state of the art. They give insight into the approaches taken by industry and academia to address GPCRs and depict how mature this target class-oriented research has become in the last decade. The book reflects the actual trends in the fast-emerging field of GPCR research in academia and industry. Front Matter....Pages i-xvii G-Proteins and GPCRs: From the Beginning....Pages 1-22 Modeling GPCRs....Pages 23-48 QSAR Modeling of GPCR Ligands: Methodologies and Examples of Applications....Pages 49-74 Privileged Structures in GPCRs....Pages 75-92 Designing Compound Libraries Targeting GPCRs....Pages 93-104 The Role of GPCR Dimerisation/Oligomerisation in Receptor Signalling....Pages 145-162 Deorphanization of G-Protein-Coupled Receptors....Pages 163-186 Virus-Encoded G-Protein-Coupled Receptors: Constitutively Active (Dys)Regulators of Cell Function and Their Potential as Drug Target....Pages 187-210 Modulation of GPCR Conformationsby Ligands, G-Proteins, and Arrestins....Pages 211-228 High Content Screening to Monitor G Protein-Coupled Receptor Internalisation....Pages 229-248 High-Throughput Lead Finding and Optimisation for GPCR Targets....Pages 249-266
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