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The Future of GPCRs in Drug Discovery: Novel technologies, leading companies, and opportunities for target expansion
Date:10/31/2011

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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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