Based on the international workshop GPCRs: From Deorphanisation to Lead Structure Identification, 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.

G Proteins and GPCR: From the Beginning

Modelling GPCRs
Privileged Structures in GPCRs
Designing Compound Libraries Targeting GPCRs
Virus-encoded G Protein Coupled Receptors: Constitutively Active (dys) Regulators of Cell Function and their Potential as Drug Target
Modulation of GPCR Conformations by Ligands, G Proteins and Arrestins
The Role of GPCR Dimerisation/Oligomerisation in Receptor Signalling
Orphan Seven Transmembrane Receptor (7TMR) Screening
High Content Screening to Monitor G Protein-Coupled Receptor Internalization
High Throughput Lead Finding and Optimisation for GPCR Targets.