Contents

Chapter 1 Introduction 1

Kenneth H. Lundstrom and Mark L. Chiu

Chapter 2 Biology of G Protein-Coupled Receptors 3

Kenneth H. Lundstrom

Chapter 3 G Protein-Coupled Receptors as Targets for Drug Discovery 15

Timothy A. Esbenshade

Chapter 4 G Protein-Coupled Receptors as Cardiovascular Drug Targets 37

Mika Scheinin and Amir Snapir

Chapter 5 G Protein-Coupled Receptors and Cancer 53

Martine J. Smit and Remko A. Bakker

Chapter 6 G Protein-Coupled Receptors in Metabolic Disease 85

Regina M. Reilly and Christine A. Collins

Chapter 7 G Protein-Coupled Receptors in CNS Drug Discovery 109

Rita Raddatz and Deborah S. Hartman

Chapter 8 Recombinant G Protein-Coupled Receptors for Drug

Discovery 143

Kenneth H. Lundstrom

Chapter 9 High Throughput Screening Assays for G Protein-Coupled

Receptors 159

Usha Warrior, Sujatha Gopalakrishnan, Jurgen Vanhauwe, and David Burns

Chapter 10 Molecular Bioinformatics of Receptor Binding and Activation 191

Kevan P. Willey, Heike Obermann, and James B. Procter

Chapter 11 Structures and Dynamics of G Protein-Coupled Receptors 227

Judith Klein-Seetharaman and Michèle C. Loewen

Chapter 12 Toward Crystallization of G Protein-Coupled Receptors 271

Mark L. Chiu and Maria P. MacWilliams

Chapter 13 Novel Solid-State NMR Methods for Structural Studies on G Protein-Coupled Receptors 297

Adam Lange and Marc Baldus

Chapter 14 Structural Genomics Initiatives 315

Kenneth H. Lundstrom

Chapter 15 Molecular Basis of Dimerization of Family A

G Protein-Coupled Receptors 325

Graeme Milligan

Chapter 16 Orphan Receptors: Promising Targets for Drug Discovery 337

Yumiko Saito, Zhiwei Wang, and Olivier Civelli

Index 357

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