Table 1.
Human Class B GPCR’s and Their Peptide Ligands
| Receptor | Peptide Ligand | Principal Biological Action | Major Disease Indication | Peptide Therapeutic | Refs. |
|---|---|---|---|---|---|
| CRF1 | CRF UCN 1 |
Stress responses Stress responses |
Depression (antagonist) | [2,43, 92] | |
| CRF2 | UCN 1 UCN 2 UCN 3 |
Stress responses Cardiac contractility Hearing |
Heart failure (agonist) | [2] | |
| GHRH | GHRH | Growth hormone release | [52,77] | ||
| GIP | GIP | Insulin secretion | Type 2 diabetes (agonist) | [52,77] | |
| Glucagon | Glucagon | Glucose homeostasis | Type 2 diabetes (antagonist) | [52,77] | |
| GLP-1 | GLP-1 | Insulin secretion | Type 2 diabetes (agonist) | Byetta (Exanatide) | [19,52,77] |
| GLP-2 | GLP-2 | Gut mucosal growth | [52,77] | ||
| PTH1 | PTH PTHrP |
Ca2+ homeostasis Developmental regulator |
Osteoporosis (agonist) | Forteo (PTH(1-34)) | [5,58,73, 90] |
| PTH2 | TIP39 | Hypothalamic secretion,Nociception | [88] | ||
| Secretin | Secretin | Pancreatic secretion | [52,77] | ||
| VPAC1 | VIP PACAP |
Neuroendocrine functions Neuroendocrine functions |
[30,77] | ||
| VPAC2 | VIP PACAP |
Neuroendocrine functions Neuroendocrine functions |
[30,77] | ||
| PAC1 | PACAP | Neuroendocrine functions | [30,77] | ||
| Calcitonin | Calcitonin | Ca2+ homeostasis | Osteoporosis (agonist) | Miacalcin (calcitonin) | [54] |
| Calcitonin/ RAMP1 | CGRP Amylin |
Vasodilation Feeding |
Migraine (antagonist) | [57,67] | |
| Calcitonin / RAMP3 | Amylin | Feeding | [57,67] | ||
| CL / RAMP1 | CGRP | Vasodilation | [57,67] | ||
| CL / RAMP2 | Adrenomedullin | Vasodilation | [57,67] | ||
| CL / RAMP3 | Adrenomedullin CGRP |
Vasodilation Vasodilation |
[57,67] |
Abbreviations:CRF- corticotropin-releasing factor; UCN - urocortin; GHRH - growth hormone-releasing hormone; GIP - glucose-dependent insulinotropic peptide; GLP - glucago nlike peptide;PTH- parathyroidhormone;PTHrP - parathyroid hormone-related protein; TIP39 - tuberoinfundibular peptide of 39 residues; VIP - vasoactive intestinal peptide; PACAP- pituitary adenylate cyclase-activating polypeptide; CGRP - calcitonin gene-related peptide; RAMP - receptor activity modifying protein; CL - calcitonin receptor-like receptor.