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The Future of GPCRs in Drug Discovery: Novel Technologies, Leading Companies, and Opportunities for Target Expansion
Date:11/8/2010

GPR119 agonists 81

H4 antagonists 82

DP2 antagonists 82

GPR109A agonists 83

GPBA agonists 84

New indications 85

Diabetes 85

Obesity 86

Osteoporosis 86

COPD 87

Alzheimer's disease 87

Chapter 6 Specialist company profiles 92

Summary 92

Introduction 92

7TM Pharma 93

Actelion 94

Acure Pharma 95

Addex Pharmaceuticals 95

Arena Pharmaceuticals 97

Ascent Therapeutics 98

Cara Therapeutics 99

Compugen 99

Dimerix Bioscience 100

DiscoveRx 100

Domain Therapeutics 100

Euroscreen 101

Galapagos 102

Heptahelix 103

Heptares Therapeutics 103

Oxagen 104

Prosarix 104

Tranzyme Pharma 105

Trevena 105

Chapter 7 Market outlook for drugs targeting GPCRs 108

Summary 108

Sustained opportunities 108

Exploited GPCRs 109

Unexploited GPCRs 110

Orphan GPCRs 111

Current treatments 111

Upcoming treatments 114

Overall assessment 117

Appendix 119

Bibliography 119

Glossary 126

Index 129

List of FiguresFigure 1.1: Commercially exploited targets by target type 22

Figure 1.2: Exploited and unexploited GPCRs by class 23

Figure 2.3: Heptahelical structure of Class A and Class B GPCRs 29

Figure 2.4: Schematic diagram of Class C GPCRs 30

Figure 2.5: GPCR signaling 32

Figure 2.6: Schematic dose response curves to different types of GPCR ligand 33

Figure 3.7: Exploitation of class A GPCRs 38

Figure 3.8: Schematic phylogenetic relationship between groups of Class A GPCRs 45

Figure 3.9: Relative exploration of groups of class A GPCRs 49

Figure 4.10: Strategic opportunities in targeting GPCRs 55

Figure 4.11: Timeline of GPCR 3-dimensional structural information 58

Figure 4.12: Potential advantages with allosteric
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