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G protein-coupled receptors (GPCRs)

G protein-coupled receptors (GPCRs) are a large family of cell membrane proteins that play a crucial role in signal transduction. They are involved in many different physiological functions and are targeted by a large percentage of currently marketed drugs, including those used to treat conditions such as hypertension, asthma, schizophrenia, and Parkinson's disease.

The basic structure of a GPCR includes seven transmembrane alpha helices, an extracellular N terminus, and an intracellular C terminus. They are called "G protein-coupled" because when they bind to their ligand (such as a hormone or neurotransmitter) on the outside of the cell, they activate an intracellular G protein. This G protein then triggers a series of downstream events inside the cell, leading to the cell's response to the original signal.

There are several different types of G proteins, and the specific G protein that a GPCR interacts with determines the downstream effects. For example, some G proteins activate enzymes that increase the production of cyclic AMP (cAMP), a common second messenger, while others inhibit this process. Other G proteins activate different signaling pathways altogether.

The GPCR family is incredibly diverse, with receptors for a wide variety of signals. These include light-sensitive receptors in the retina, smell receptors in the nose, and a wide range of hormone and neurotransmitter receptors throughout the body. Because of their involvement in so many different physiological processes, they are a major focus of pharmaceutical research.


  1. 5-Hydroxytryptamine receptors
  2. Acetylcholine receptors (muscarinic)
  3. Adenosine receptors
  4. Adhesion Class GPCRs
  5. Adrenoceptors
  6. Angiotensin receptors
  7. Apelin receptor
  8. Bile acid receptor
  9. Bombesin receptors
  10. Bradykinin receptors
  11. Calcitonin receptors
  12. Calcium-sensing receptor
  13. Cannabinoid receptors
  14. Chemerin receptors
  15. Chemokine receptors
  16. Cholecystokinin receptors
  17. Class Frizzled GPCRs
  18. Complement peptide receptors
  19. Corticotropin-releasing factor receptors
  20. Dopamine receptors
  21. Endothelin receptors
  22. G protein-coupled estrogen receptor
  23. Formylpeptide receptors
  24. Free fatty acid receptors
  25. GABABreceptors
  26. Galanin receptors
  27. Ghrelin receptor
  28. Glucagon receptor family
  29. Glycoprotein hormone receptors
  30. Gonadotrophin-releasing hormone receptors
  31. GPR18, GPR55 and GPR119
  32. Histamine receptors
  33. Hydroxycarboxylic acid receptors
  34. Kisspeptin receptor
  35. Leukotriene receptors
  36. Lysophospholipid (LPA) receptors
  37. Lysophospholipid (S1P) receptors
  38. Melanin-concentrating hormone receptors
  39. Melanocortin receptors
  40. Melatonin receptors
  41. Metabotropic glutamate receptors
  42. Motilin receptor
  43. Neuromedin U receptors
  44. Neuropeptide FF/neuropeptide AF receptors
  45. Neuropeptide S receptor
  46. Neuropeptide W/neuropeptide B receptors
  47. Neuropeptide Y receptors
  48. Neurotensin receptors
  49. Opioid receptors
  50. Orexin receptors
  51. Oxoglutarate receptor
  52. P2Y receptors
  53. Parathyroid hormone receptors
  54. Platelet-activating factor receptor
  55. Prokineticin receptors
  56. Prolactin-releasing peptide receptor
  57. Prostanoid receptors
  58. Proteinase-activated receptors
  59. QRFP receptor
  60. Relaxin family peptide receptors
  61. Somatostatin receptors
  62. Succinate receptor
  63. Tachykinin receptors
  64. Thyrotropin-releasing hormone receptors
  65. Trace amine receptor
  66. Urotensin receptor
  67. Vasopressin and oxytocin receptors
  68. VIP and PACAP receptors
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