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The Future of GPCRs in Drug Discovery: Novel technologies, leading companies, and opportunities for target expansion

NEW YORK, Oct. 31, 2011 /PRNewswire/ -- announces that a new market research report is available in its catalogue:

The Future of GPCRs in Drug Discovery: Novel technologies, leading companies, and opportunities for target expansion

G-Protein-coupled receptors (GPCRs) constitute the largest family of membrane receptors, and the pharmaceutical industry has targeted them to a greater extent than any other protein class. Despite the high revenues generated by branded drugs that are active at GPCRs, only a small fraction of the GPCR family has thus far been commercially exploited. Consequently, considerable scope exists for broadening the reach of drug discovery efforts to counteract the impending patent expiries of many of the best-selling GPCR-targeted drugs.

This report provides insight into how recent advances in the understanding of GPCR function are opening up new avenues for exploration, where the most promising opportunities lie, and which companies are best placed to advance their GPCR-based proprietary drug discovery technologies. The report begins with outlines of the current commercial status of drugs targeting GPCRs and the scientific basis of their action, offering an understanding of why the large majority of the receptor family has remained unexploited.

This is followed by discussion of the scientific developments enabling the pursuit of new approaches such as allosteric modulation, bifunctional ligand design, and the targeting of dimeric receptors. Both old and new targets are considered in terms of their potential to offer fresh opportunities, and particular attention is given to the current and future roles of orphan receptors. Finally, the report profiles a range of companies specializing in aspects of GPCR drug discovery, and the market outlook is summarized.

List of Tables

The Future of GPCRs in Drug Discovery

Executive summary 10

Introduction 10

Characteristics of GPCRs 10

Commercial exploitation 11

New approaches 12

New opportunities 13

Specialist company profiles 14

Market outlook for dugs targeting GPCRs 14

Chapter 1 Introduction 18

Summary 18

Introduction 18

GPCRs in the human genome 19

Additional opportunities 20

The leading class of drug targets 21

Commercially validated targets 23

Chapter 2 Characteristics of GPCRs 28

Summary 28

Introduction 28

Protein structure 29

Functional receptors 31

Second messengers 31

Agonists, antagonists, partial agonists, and inverse agonists 33

Chapter 3 Commercial exploitation 36

Summary 36

Introduction 37

Current successes 37

Targeted GPCRs 44

Unexplored targets 47

Difficult targets 50

Opportunities 50

Chapter 4 New approaches 54

Summary 54

Introduction 55

Screening methods 56

Structure-based methods 57

Knowledge-based methods 60

Allosteric modulators 62

Bifunctional ligands 65

Dimeric receptor targeting ligands 66

Biased ligands 68

Chapter 5 New opportunities 72

Summary 72

Introduction 73

Enhanced selectivity 73

Atypical antipsychotics 75

Lorcaserin 78

Adenosine A2A antagonists 79

New targets 80

Ghrelin antagonists 81

GPR119 agonists 81

H4 antagonists 82

DP2 antagonists 82

GPR109A agonists 83

GPBA agonists 84

New indications 85

Diabetes 85

Obesity 86

Osteoporosis 86


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 Figures

Figure 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 modulators of GPCR function 62

Figure 4.13: Schematic of allosteric modulator approach 63

Figure 4.14: Comparison of biased ligands and conventional GPCR ligands 69

Figure 5.15: Approach to more selective antipsychotic drugs 76

Figure 5.16: Lorcaserin, enhanced 5-HT2C receptor selectivity 78

Figure 7.17: Continued opportunities to exploit GPCRs 109

Figure 7.18: Angiotensin AT1 antagonists - the patent cliff in the US 113

List of Tables

Table 1.1: Classes of GPCRs 19

Table 1.2: Sales of GPCR-directed drugs achieving sales of >$250m in 2009 24

Table 3.3: Sales of AT1 receptor antagonists ($m), 2009 42

Table 5.4: GPR119 agonists in development for the treatment of type 2 diabetes 82

Table 5.5: DP2 antagonists in development for the treatment of asthma 83

Table 6.6: GPCR pipeline of 7TM Pharma 93

Table 6.7: GPCR pipeline of Actelion 94

Table 6.8: GPCR pipeline of Addex Pharmaceuticals 96

Table 6.9: GPCR pipeline of Arena Pharmaceuticals 97

Table 6.10: GPCR pipeline of Domain Therapeutics 101

Table 6.11: GPCR pipeline of Euroscreen 102

Table 6.12: GPCR pipeline of Tranzyme Pharma 105

Table 7.13: Drugs in advanced development, targeting unexploited GPCRs 115

Companies mentioned

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Drug Discovery and Development Industry: The Future of GPCRs in Drug Discovery: Novel technologies, leading companies, and opportunities for target expansion

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Nicolas Bombourg
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Intl: +1 805-652-2626

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