Class II G protein-coupled receptors for VIP and PACAP: structure, models of activation and pharmacology.
VIP and PACAP impact strongly on human pathophysiology. Their receptors are very promising targets for developing new drugs in the treatment of inflammatory and neurodegenerative diseases. This article reviews the present knowledge regarding VIP and PACAP receptors, i.e. VPAC1, VPAC2 and PAC1. This includes: (I) a critical review of instrumental peptide agonists and antagonists; (II) a survey of recent data regarding the structure of VPAC1 receptor and the docking of VIP in the receptor binding domain. Structural models for the VPAC2 and PAC1 receptor N-terminal ectodomains are also described; (III) A critical description of the two models of VPAC1 receptor activation in the general context of class II/family B G protein-coupled receptors.
Laburthe
Marc
M
INSERM, U773, Centre de Recherche Biomédicale Bichat Beaujon, CRB3, Université Paris 7 Denis Diderot, BP416, F-75018 Paris, France. laburthe@bichat.inserm.fr
Couvineau
Alain
A
Tan
Var
V
D000595:Amino Acid Sequence; D000818:Animals; D006801:Humans; D008958:Models, Molecular; D008969:Molecular Sequence Data; D017434:Protein Structure, Tertiary; D051237:Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I / Q000819:agonists / Q000037:antagonists & inhibitors / Q000737:chemistry*; D051239:Receptors, Vasoactive Intestinal Peptide, Type II / Q000819:agonists / Q000037:antagonists & inhibitors / Q000737:chemistry*; D051238:Receptors, Vasoactive Intestinal Polypeptide, Type I / Q000819:agonists / Q000037:antagonists & inhibitors / Q000737:chemistry*; D017386:Sequence Homology, Amino Acid
D051237:Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I; D051239:Receptors, Vasoactive Intestinal Peptide, Type II; D051238:Receptors, Vasoactive Intestinal Polypeptide, Type I