G protein-coupled receptors (GPCRs) are important conformational "switches" in transmembrane signal transduction and represent the largest gene family in the human genome reflecting the importance of GPCRs as targets for hormones, neurotransmitters and local mediators in virtually any cell type of the human body. Since GPCRs discriminate well between natural and synthetic ligands and because of their localization in the plasma membrane, they are the single most important class of drug targets.
With its particular emphasis on the constitutive activity of GPCRs, this book recognizes a biological process that has not yet been covered by existing books on GPCRs. An international team of highly distinguished authors discusses current models and concepts in detail, introducing the advances made in our understanding GPCR activation and constitutive activity. In addition, the text provides an overview on the methods of investigating GPCR activity.

From the contents:
PART I: GENERAL CONCEPTS
Models of constitutive activity
Molecular mechanisms of GPCR activation
Impact of G proteins on constitutive GPCR activity
Physiological and therapeutic relevance of constitutive GPCR activity
Methodological Approaches
PART II: SELECTED GPCR SYSTEMS
Chemokine receptors and human disease
a-Adrenoceptors
ß-Adrenoceptors
Muscarinic Acetylcholine Receptors
Histamine receptors
5-HT receptors
Virally pirated Chemokine receptors and human disease

Illustrated by numerous experimental examples, schemes and methodological advice for analyzing GPCRs, this is a highly practical reference for pharmaceutical chemists, physiologists and medical researchers in academia and industry.