Current advances in functional screening methodologies, medicinal chemistry, and structure-based drug design have generated large increases in the number and diversity of GPCR drug targets. Furthermore, basic research advances have opened the way for still further exploitation of this target class. This report:Explores current and likely consequences of recent advances concerning GPCR x-ray structures, allosteric interactions, multimerization, and functional selectivity; Extensively tabulates marketed drugs and compounds in development arranged by receptor type and subtype; Presents in-depth interviews with recognized experts in the field. G protein-coupled receptors (GPCRs) are popular drug targets, accounting for about one-third of approved drugs and many hundreds of drugs currently in development. Yet one can easily argue that the pharmacologic potential of GPCRs is far from exhausted. Currently approved drugs address only a few GPCRs. Technologic and scientific advances have resulted in R&D pipelines that target a great many more GPCRs than are represented among currently marketed products. In this report, we examine newer technologies used in GPCR pharmacology.  

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GPCRs: Dawn of a New Era'
Published on October 2008
Report Summary
Current advances in functional screening methodologies, medicinal chemistry, and structure-based drug design have generated large
increases in the number and diversity of GPCR drug targets. Furthermore, basic research advances have opened the way for still
further exploitation of this target class.
This report:Explores current and likely consequences of recent advances concerning GPCR x-ray structures, allosteric interactions,
multimerization, and functional selectivity; Extensively tabulates marketed drugs and compounds in development arranged by
receptor type and subtype; Presents in-depth interviews with recognized experts in the field. G protein-coupled receptors (GPCRs)
are popular drug targets, accounting for about one-third of approved drugs and many hundreds of drugs currently in development. Yet
one can easily argue that the pharmacologic potential of GPCRs is far from exhausted. Currently approved drugs address only a few
GPCRs. Technologic and scientific advances have resulted in R&D pipelines that target a great many more GPCRs than are
represented among currently marketed products. In this report, we examine newer technologies used in GPCR pharmacology.
Table of Content
Chapter 1INTRODUCTION: THE UNTAPPED PHARMACOLOGIC POTENTIAL OF GPCRS1.1. Research Advances Stimulating
GPCR-Based Drug Discovery1.2. Goals and Organization of ReportChapter 2SCIENTIFIC BACKGROUND AND
TECHNOLOGIES2.1. Nature of GPCRsGPCRs as Drug TargetsGPCR Classification2.2. Compound SelectionFunctional Assays for
GPCR Signaling Calcium Assays Cellular Dielectric Spectroscopy Beta-Arrestin AssaysStructure-Based Drug Discovery
Chapter 3GPCR PHARMACOLOGY: KEY ADVANCES IN BASIC RESEARCH3.1. Significance of GPCR StructuresX-Ray
Crystallographic Structure of the Beta2-Adrenergic Receptor…SolvedImplications for Structure-Based Drug Design for
GPCRs3.2. Deorphanization3.3. Allosteric Modulators3.4. Dimers and Oligomers3.5. Functional SelectivityChapter 4APPLIED
RESEARCH4.1. Small Companies Push the Limits of GPCR Pharmacology7TM PharmaAcadia
PharmaceuticalsActelionAcurePharmaAddex PharmaceuticalsAdenosine Therapeutics (Acquired by Clinical Data)Arena
PharmaceuticalsCara TherapeuticsDimerix BioscienceEPIX PharmaceuticalsTrevena4.2. The GPCR PipelineSerotonin Receptors
5-HT1 Receptor 5-HT2 Receptor 5-HT4 to 5-HT7 ReceptorsAdenosine Receptors A1 Receptor A2 and A3
ReceptorsAdrenergic Receptors Alpha Adrenergic Receptor Beta Adrenergic ReceptorAngiotensin II ReceptorArginine
Vasopressin ReceptorBradykinin ReceptorsCalcitonin ReceptorsCannabinoid ReceptorChemokine ReceptorsCholecystokinin
ReceptorMuscarinic Acetylcholine ReceptorCoagulation Factor II ReceptorCorticotropin-Releasing Hormone Receptor 1Dopamine
ReceptorsEndothelin Receptor Type AGABAB ReceptorGlucagon Receptor FamilyMetabotropic Glutamate
ReceptorsGonadotropin-Releasing Hormone ReceptorGhrelin ReceptorHistamine ReceptorInterleukin 8
ReceptorMelanin-Concentrating Hormone Receptor 1Melanocortin ReceptorMotilin ReceptorOpiate Receptor-Like 1 and Opioid
ReceptorsOxytocin ReceptorProstaglandin ReceptorsGPCR44Purinergic P2Y ReceptorsSphingosine-1-Phosphate Receptor
1Tachykinin ReceptorsAdditional GPCR ModulatorsChapter 5DEALS, OBSERVATIONS, AND CONCLUSIONS5.1. Selected
GPCR-Related Deals5.2. Strengths and Weaknesses of GPCRs as a Target ClassStrengthsWeaknesses5.3. General Observations
and FindingsDiversity of GPCRs for Drug Discovery and DevelopmentTranslation of Basic Research and New
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TechnologiesFunctional Versus Ligand-Binding Screening Assays Cell Impedance Screening TechnologyRole of Allostery in Drug
Discovery and DevelopmentRole of Dimers and Oligomers in Drug Discovery and DevelopmentRelationship of Signaling Pathway to
DiseaseDeorphanization and Unfamiliar GPCRsStructure-Based Drug Design5.4. ConclusionsChapter 6EXPERT INTERVIEWS6.1.
Annette Gilchrist, PhDAdjunct Professor; Northwestern University6.2. Graeme Milligan, PhDProfessor of Molecular Pharmacology;
Joint Research Director, Faculty of Biomedical and Life Sciences; University of Glasgow6.3. AnonymousScreening and Profiling
Director; Major Pharmaceutical Company X6.4. P. Jeffrey Conn, PhDLee E. Limbird Professor of Pharmacology; Director, Vanderbilt
Program in Drug Discovery; Vanderbilt University Medical Center6.5. Sidney Topiol, PhDAssociate Director, Computational
Chemistry; Lundbeck Research6.6. Vincent Mutel, PhDCEO, Vice Chairman, and Co-Founder; Addex PharmaceuticalsFIGURES
Figure 2.1. Diagram of a FLIPR Instrument and Typical Kinetic TracingsFigure 2.2. Crystal Structure of the Beta2-Adrenergic
Receptor ProteinTABLESTable 2.1. Major GPCR SubclassesTable 4.1. Launched Drugs Targeting Serotonin 1 ReceptorsTable 4.2.
Drug Candidates for Serotonin 1 ReceptorsTable 4.3. Launched Drugs Targeting Serotonin 2 ReceptorsTable 4.4. Drug Candidates
for Serotonin 2 ReceptorsTable 4.5. Launched Drugs Targeting Serotonin 4 ReceptorsTable 4.6. Drug Candidates for Serotonin 4
ReceptorsTable 4.7. Drug Candidates for Serotonin 5, 6, and 7 ReceptorsTable 4.8. Drug Candidates for Adenosine A1
ReceptorsTable 4.9. Drug Candidates for Adenosine A2 and A3 ReceptorsTable 4.10. Launched Drugs Targeting Alpha Adrenergic
ReceptorsTable 4.11. Drug Candidates for Alpha Adrenergic ReceptorsTable 4.12. Launched Drugs Targeting Beta-1 Adrenergic
ReceptorsTable 4.13. Drug Candidates for Beta-1 Adrenergic ReceptorsTable 4.14. Launched Drugs Targeting Beta-2 Adrenergic
ReceptorsTable 4.15. Drug Candidates for Beta-2 Adrenergic ReceptorsTable 4.16. Drug Candidates for Beta-3 Adrenergic
ReceptorsTable 4.17. Launched Drugs Targeting Angiotensin II Receptor, Type 1Table 4.18. Drug Candidates for Arginine
Vasopressin ReceptorsTable 4.19. Drug Candidates for Bradykinin ReceptorsTable 4.20. Drug Candidates for Calcitonin and
Calcitonin-Like ReceptorsTable 4.21. Preclinical Drug Candidates for Cannabinoid 1 ReceptorsTable 4.22. Clinical Drug Candidates
for Cannabinoid 1 ReceptorsTable 4.23. Drug Candidates for Cannabinoid 2 ReceptorsTable 4.24. Drug Candidates for Chemokine
ReceptorsTable 4.25. Drug Candidates for Cholecystokinin ReceptorsTable 4.26. Launched Drugs Targeting Muscarinic Receptor
1Table 4.27. Drug Candidates for Muscarinic 1 and 2 Cholinergic ReceptorsTable 4.28. Launched Drugs Targeting Muscarinic
Receptor 3Table 4.29. Drug Candidates for Muscarinic 3 Cholinergic ReceptorsTable 4.30. Drug Candidates for Coagulation Factor II
ReceptorTable 4.31. Drug Candidates for Corticotropin-Releasing Hormone ReceptorsTable 4.32. Launched Drugs Targeting the
Dopamine D2 ReceptorTable 4.33. Drug Candidates for Dopamine ReceptorsTable 4.34. Drug Candidates for Endothelin Receptor
Type ATable 4.35. Drug Candidates for GABAB ReceptorsTable 4.36. Drug Candidates for Glucagon and Glucagon-Like Peptide-1
ReceptorsTable 4.37. Drug Candidates for Metabotropic Glutamate ReceptorsTable 4.38. Launched Drugs Targeting the
Gonadotropin-Releasing Hormone ReceptorTable 4.39. Drug Candidates for the Gonadotropin-Releasing Hormone ReceptorTable
4.40. Drug Candidates for Ghrelin (aka Growth Hormone Secretagogue) ReceptorsTable 4.41. Launched Drugs Targeting the
Histamine H1 and H2 ReceptorsTable 4.42. Drug Candidates for Histamine ReceptorsTable 4.43. Drug Candidates for Interleukin 8
ReceptorsTable 4.44. Drug Candidates for Melanin-Concentrating Hormone Receptor 1Table 4.45. Drug Candidates for Melanocortin
ReceptorsTable 4.46. Drug Candidates for the Motilin ReceptorTable 4.47. Drug Candidates for Opiate Receptor-Like 1; Also for
Delta 1 and Kappa 1 Opioid ReceptorsTable 4.48. Drug Candidates for Opioid Receptors Mu and SigmaTable 4.49. Drug Candidates
for the Oxytocin ReceptorTable 4.50. Launched Drugs Targeting Prostaglandin ReceptorsTable 4.51. Drug Candidates for
Prostaglandin ReceptorsTable 4.52. Drug Candidates for GPCR 44Table 4.53. Drug Candidates for Purinergic ReceptorsTable 4.54.
Drug Candidates for Sphingosine-1-Phosphate Receptor 1Table 4.55. Drug Candidates for Tachykinin ReceptorsTable 4.56.
Launched Drugs Targeting Miscellaneous GPCRsTable 4.57. Miscellaneous GPCR-Targeted Drugs in DevelopmentTable 5.1.
Selected Recent GPCR Candidate-Compound-Related Deals
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