Table 1.
Summary of Family B GPCR physiology and drugs (Hoare, 2005; Archbold et al., 2011; Bortolato et al., 2014).
| Receptor(s) | Ligands | Physiological functions | Disease(s) | Available drugs |
|---|---|---|---|---|
| CALCITONIN RECEPTOR FAMILY | ||||
| Calcitonin receptor (CTR) | Calcitonin | Ca2+ homeostasis | Osteoporosis | Miacalcin, Fortical |
| Amylin receptors (AMY1, AMY2, AMY3) | Amylin | Energy homeostasis and body fluid balance | Diabetes/obesity | Pramlintide |
| Amyloid-beta (Aβ) protein | ||||
| Calcitonin gene-related peptide receptor (CGRP receptor) | α-calcitonin gene-related peptide (α-CGRP) | Vasodilation and nociception | Migraine | |
| ß-CGRP | ||||
| Adrenomedullin receptors (AM1, AM2) | adrenomedullin 1 | Vasodilation | Cardiovascular disease, cancer | |
| adrenomedullin 2 | ||||
| GLUCAGON RECEPTOR FAMILY | ||||
| Glucagon receptor (GCGR) | Glucagon | Regulation of blood glucose | Diabetes | Glucagon |
| Glucagon-like peptide 1 receptor (GLP-1R) | Glucagon-like peptide 1 (GLP-1) | Insulin and glucagon secretion | Diabetes | Exenatide, Lixisenatide, Liraglutide, Albiglutide, Dulaglutide |
| Glucagon-like peptide 2 receptor (GLP-2R) | Glucagon-like peptide 2 (GLP-2) | Gut mucosal growth | Short bowel syndrome, Crohn's disease, osteoporosis | Teduglutide |
| Gastric inhibitory polypeptide receptor (GIPR) | Gastric inhibitory polypeptide (GIP) | Insulin secretion, fatty acid metabolism | Diabetes/obesity | |
| CORTICOTROPIN-RELEASING HORMONE RECEPTORS | ||||
| Corticotropin-releasing factor receptor 1 (CRF1R) | Corticotropin-releasing factor (CRF) | Release of ACTH and central stress responses | Stress, inflammatory bowel syndrome | Corticorelin |
| Urocortin I (Ucn1) | ||||
| Corticotropin-releasing factor receptor 2 (CRF2R) | CRF | Central stress responses, cardiac contractility, hearing | Cancer, heart failure, hypertension | |
| Urocortin II (Ucn2) | ||||
| Urocortin III (Ucn3) | ||||
| PARATHYROID HORMONE RECEPTORS | ||||
| Parathyroid hormone 1 receptor (PTH1R) | Parathyroid hormone (PTH) | Ca2+ homeostasis | Osteoporosis, hypoparathyroidism | Teriparatide, Preotact |
| Parathyroid hormone-related protein (PTHrP) | Developmental regulator | |||
| Parathyroid hormone 2 receptor (PTH2R) | PTH | Hypothalamic secretion, nociception | Nociception | |
| Tuberoinfundibular peptide of 39 residues (TIP39) | ||||
| VASOACTIVE INTESTINAL POLYPEPTIDE RECEPTORS | ||||
| Vasoactive intestinal polypeptide receptor 1 (VPAC1R) | Vasoactive intestinal polypeptide (VIP) | Vasodilation, neurotransmission, neuroendocrine functions | Inflammation, neurodegeneration | |
| PACAP | ||||
| Vasoactive intestinal polypeptide receptor 2 (VPAC2R) | VIP | Vasodilation, neurotransmission neuroendocrine functions | Inflammation, neurodegeneration | |
| PACAP | ||||
| OTHERS | ||||
| Pituitary adenylate cyclase-activating polypeptide type I receptor (PAC1R) | Pituitary adenylate cyclase-activating polypeptide (PACAP) | Neurotransmission neuroendocrine functions | Neurodegeneration nociception, glucose homeostasis | |
| Growth-hormone-releasing hormone receptor (GHRHR) | Growth hormone-releasing hormone (GRHR) | Release of growth hormone | Dwarfism, HIV-related lipodystrophy | Tesamorelin, Sermorelin, CJC-1295 |
| Secretin receptor (SCTR) | Secretin | Pancreatic secretion | Autism, schizophrenia, duodenal ulcers, gastrinoma | |