Molecular pharmacology and structure of VPAC Receptors for VIP and PACAP.
VIP and PACAP are two prominent neuropeptides which share two common G protein-coupled receptors VPAC1 and VPAC2 while PACAP has an additional specific receptor PAC1. This paper reviews the present knowledge regarding three aspects of VPAC receptors including: (i). receptor specificity towards natural VIP-related peptides and pharmacology of synthetic agonists or antagonists; (ii). receptor signaling; (iii). molecular basis of ligand-receptor interaction as determined by site-directed mutagenesis, construction of receptor chimeras and structural modeling.
Laburthe
M
M
Neuroendocrinology and Cell Biology, INSERM U41O, Faculté de Médecine Xavier Bichat, 75018, Paris, France. laburhe@bichat.inserm.fr
Couvineau
A
A
D000595:Amino Acid Sequence; D000818:Animals; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D009479:Neuropeptides / Q000502:physiology*; D051219:Pituitary Adenylate Cyclase-Activating Polypeptide; D011487:Protein Conformation; D051236:Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide; D051237:Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I; D011979:Receptors, Pituitary Hormone / Q000502:physiology*; D018005:Receptors, Vasoactive Intestinal Peptide / Q000737:chemistry / Q000502:physiology*; D051239:Receptors, Vasoactive Intestinal Peptide, Type II; D051238:Receptors, Vasoactive Intestinal Polypeptide, Type I; D013379:Substrate Specificity; D014660:Vasoactive Intestinal Peptide / Q000737:chemistry / Q000378:metabolism*
C495401:ADCYAP1 protein, human; C495503:ADCYAP1R1 protein, human; D008024:Ligands; D009479:Neuropeptides; D051219:Pituitary Adenylate Cyclase-Activating Polypeptide; D051236:Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide; D051237:Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I; D011979:Receptors, Pituitary Hormone; D018005:Receptors, Vasoactive Intestinal Peptide; D051239:Receptors, Vasoactive Intestinal Peptide, Type II; D051238:Receptors, Vasoactive Intestinal Polypeptide, Type I; C495506:VIPR1 protein, human; C495509:VIPR2 protein, human; D014660:Vasoactive Intestinal Peptide