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. 2012 Jan 23;33(3):300–311. doi: 10.1038/aps.2011.170

Table 1. An overview of secretin receptor family members and their ligands, with structural details and therapeutic applications.

Secretin family receptor Cognate ligands ECD-PDB Physiological relevance Disorders Therapeutic drugs
CRFR1 CRF, Urocortin1 3EHS, 3EHU11, 2L2713, Stress related pathway Depression/Anxiety Corticorelin/ Acthrel (approved)
CRFR2α CRF, Urocortin1, Urocortin2, Urocortin3 1U345, 2JND6, 3N96, 3N95, 3N9314 Stress related pathway, Cardiac contractility, Angiogenesis Depression/Anxiety, Heart failure, Cancer  
PTH1R PTH, PTHrP 3L2J 39, 3C4M10, 3H3G12 Ca2+ homeostasis Hyperparathyroidism Osteoporosis Forteo (approved) Preotact (approved in Europe)
PTH2R PTH, Tip39 Hypothalamic secretion, Nociception    
GHRH receptor GHRH Growth hormone secretion Dwarfism Tesamorelin (approved)
Glucagon receptor Glucagon Glucose homeostasis Type 2 diabetes  
GLP1 receptor GLP-1, Exendin4 3IOL76, 3C599 Insulin secretion Type 2 diabetes Byetta/Exenatide, Liraglutide (both approved)
GLP-2 receptor GLP-2   Glucagon secretion, Gut mucosal growth Short bowel syndrome Teduglutide (Phase III)
GIP receptor GIP 2QKH7 Insulin secretion Lipid metabolism Type 2 diabetes
PAC1R PACAP, VIP 3N9416, 2JOD8 Neurotransmitter, Neuromodulator, Neuroprotection Schizophrenia, Medulloblastoma
VPAC1R VIP, PACAP Vasodilation, Digestion, Neuroprotection Crohn's disease, rheumatoid arthritis
VPAC2R VIP, PACAP 2X57 Vasodilation, Digestion, Neuroprotection Schizophrenia
Secretin receptor Secretin Pancreatic secretin H2O homeostasis  
Calcitonin receptor Calcitonin - Ca2+ homeostasis Osteoporosis Miacalcin, Cibacalcin (approved)
AMY receptor (CTR /RAMP1,2,3) Amylin   Glucose homeostasis Diabetes Pramlintide/Smylin (approved)
CGRP receptor (CLR/RAMP1) CGRP 3N7S15 Vasodilation Migraine Telcagepant (Phase III fail)
AM1 receptor (CLR/RAMP2) Andromedulin 2XVT (RAMP2) Circulatory system, Vasodilation Cardiovascular disease  
AM2 receptor (CLR/RAMP3) CGRP, Andromedulin   Vasodilation, Cellular tolerance for oxidative stress Cardiovascular diseases