GPCRs: Dawn of a New Era?
Author: Ken Rubenstein, PhD
FIGURES
Figure 2.1. Diagram of a FLIPR Instrument and Typical Kinetic Tracings
Figure 2.2. Crystal Structure of the Beta2-Adrenergic Receptor Protein
TABLES
Table 2.1. Major GPCR Subclasses
Table 4.1. Launched Drugs Targeting Serotonin 1 Receptors
Table 4.2. Drug Candidates for Serotonin 1 Receptors
Table 4.3. Launched Drugs Targeting Serotonin 2 Receptors
Table 4.4. Drug Candidates for Serotonin 2 Receptors
Table 4.5. Launched Drugs Targeting Serotonin 4 Receptors
Table 4.6. Drug Candidates for Serotonin 4 Receptors
Table 4.7. Drug Candidates for Serotonin 5, 6, and 7 Receptors
Table 4.8. Drug Candidates for Adenosine A1 Receptors
Table 4.9. Drug Candidates for Adenosine A2 and A3 Receptors
Table 4.10. Launched Drugs Targeting Alpha Adrenergic Receptors
Table 4.11. Drug Candidates for Alpha Adrenergic Receptors
Table 4.12. Launched Drugs Targeting Beta-1 Adrenergic Receptors
Table 4.13. Drug Candidates for Beta-1 Adrenergic Receptors
Table 4.14. Launched Drugs Targeting Beta-2 Adrenergic Receptors
Table 4.15. Drug Candidates for Beta-2 Adrenergic Receptors
Table 4.16. Drug Candidates for Beta-3 Adrenergic Receptors
Table 4.17. Launched Drugs Targeting Angiotensin II Receptor, Type 1
Table 4.18. Drug Candidates for Arginine Vasopressin Receptors
Table 4.19. Drug Candidates for Bradykinin Receptors
Table 4.20. Drug Candidates for Calcitonin and Calcitonin-Like Receptors
Table 4.21. Preclinical Drug Candidates for Cannabinoid 1 Receptors
Table 4.22. Clinical Drug Candidates for Cannabinoid 1 Receptors
Table 4.23. Drug Candidates for Cannabinoid 2 Receptors
Table 4.24. Drug Candidates for Chemokine Receptors
Table 4.25. Drug Candidates for Cholecystokinin Receptors
Table 4.26. Launched Drugs Targeting Muscarinic Receptor 1
Table 4.27. Drug Candidates for Muscarinic 1 and 2 Cholinergic Receptors
Table 4.28. Launched Drugs Targeting Muscarinic Receptor 3
Table 4.29. Drug Candidates for Muscarinic 3 Cholinergic Receptors
Table 4.30. Drug Candidates for Coagulation Factor II Receptor
Table 4.31. Drug Candidates for Corticotropin-Releasing Hormone Receptors
Table 4.32. Launched Drugs Targeting the Dopamine D2 Receptor
Table 4.33. Drug Candidates for Dopamine Receptors
Table 4.34. Drug Candidates for Endothelin Receptor Type A
Table 4.35. Drug Candidates for GABAB Receptors
Table 4.36. Drug Candidates for Glucagon and Glucagon-Like Peptide-1 Receptors
Table 4.37. Drug Candidates for Metabotropic Glutamate Receptors
Table 4.38. Launched Drugs Targeting the Gonadotropin-Releasing Hormone Receptor
Table 4.39. Drug Candidates for the Gonadotropin-Releasing Hormone Receptor
Table 4.40. Drug Candidates for Ghrelin (aka Growth Hormone Secretagogue) Receptors
Table 4.41. Launched Drugs Targeting the Histamine H1 and H2 Receptors
Table 4.42. Drug Candidates for Histamine Receptors
Table 4.43. Drug Candidates for Interleukin 8 Receptors
Table 4.44. Drug Candidates for Melanin-Concentrating Hormone Receptor 1
Table 4.45. Drug Candidates for Melanocortin Receptors
Table 4.46. Drug Candidates for the Motilin Receptor
Table 4.47. Drug Candidates for Opiate Receptor-Like 1; Also for Delta 1 and Kappa 1 Opioid Receptors
Table 4.48. Drug Candidates for Opioid Receptors Mu and Sigma
Table 4.49. Drug Candidates for the Oxytocin Receptor
Table 4.50. Launched Drugs Targeting Prostaglandin Receptors
Table 4.51. Drug Candidates for Prostaglandin Receptors
Table 4.52. Drug Candidates for GPCR 44
Table 4.53. Drug Candidates for Purinergic Receptors
Table 4.54. Drug Candidates for Sphingosine-1-Phosphate Receptor 1
Table 4.55. Drug Candidates for Tachykinin Receptors
Table 4.56. Launched Drugs Targeting Miscellaneous GPCRs
Table 4.57. Miscellaneous GPCR-Targeted Drugs in Development
Table 5.1. Selected Recent GPCR Candidate–Compound-Related Deals