VPAC receptors for VIP and PACAP.
VIP and PACAP are two prominent neuropeptides that share two common G protein-coupled receptors, VPAC1 and VPAC2, while PACAP has an additional specific receptor, PAC1. This article reviews the present knowledge regarding various aspects of VPAC receptors including: 1) receptor specificity toward natural VIP-related peptides and pharmacology of synthetic agonists or antagonists; 2) genomic organization and chromosomal localization; 3) signaling and established or putative interactions with G proteins or accessory proteins such as RAMPs or PDZ-containing proteins; 4) molecular basis of ligand-receptor interaction as determined by site-directed mutagenesis, construction of receptor chimeras, and structural modeling; 5) constitutively active receptor mutants; 6) short-term (desensitization, internalization, phosphorylation) and long-term (transcription) regulations and transgenic models; 7) receptor polymorphisms.
Laburthe
M
M
Neuroendocrinology and Cell Biology, INSERM U410, Faculté de Médecine, Xavier Bichat, 75018 Paris, France. laburthe@bichat.inserm.fr
Couvineau
A
A
Marie
J C
JC
D000818:Animals; D002874:Chromosome Mapping; D005786:Gene Expression Regulation / Q000502:physiology; D006801:Humans; D008024:Ligands; D051379:Mice; D009479:Neuropeptides / Q000378:metabolism* / Q000494:pharmacology; D051219:Pituitary Adenylate Cyclase-Activating Polypeptide; D011485:Protein Binding; D017433:Protein Structure, Secondary; D051381:Rats; D018005:Receptors, Vasoactive Intestinal Peptide / Q000235:genetics / Q000378:metabolism*; D051239:Receptors, Vasoactive Intestinal Peptide, Type II; D051238:Receptors, Vasoactive Intestinal Polypeptide, Type I; D011993:Recombinant Fusion Proteins / Q000235:genetics / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects* / Q000502:physiology; D014660:Vasoactive Intestinal Peptide / Q000378:metabolism* / Q000494:pharmacology
C495401:ADCYAP1 protein, human; C495402:Adcyap1 protein, mouse; C495403:Adcyap1 protein, rat; D008024:Ligands; D009479:Neuropeptides; D051219:Pituitary Adenylate Cyclase-Activating Polypeptide; D018005:Receptors, Vasoactive Intestinal Peptide; D051239:Receptors, Vasoactive Intestinal Peptide, Type II; D051238:Receptors, Vasoactive Intestinal Polypeptide, Type I; D011993:Recombinant Fusion Proteins; D014660:Vasoactive Intestinal Peptide