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 GPCRs: From the Beginning

Modeling GPCRs
QSAR Modeling of GPCR Ligands: Methodologies and Examples of Applications
Privileged Structures in GPCRs
Designing Compound Libraries Targeting GPCRs
Orphan Seven Transmembrane Receptor Screening
The Role of GPCR Dimerisation/Oligomerisation in Receptor Signalling
Deorphanization of G-Protein-Coupled Receptors
Virus-Encoded G-Protein-Coupled Receptors: Constitutively Active (Dys)Regulators of Cell Function and Their Potential as Drug Target
Modulation of GPCR Conformationsby Ligands, G-Proteins, and Arrestins
High Content Screening to Monitor G Protein-Coupled Receptor Internalisation
High-Throughput Lead Finding and Optimisation for GPCR Targets.