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Updated: Jan 12, 2026

A Pipeline to Investigate the Structures and Signaling Pathways of Sphingosine 1-Phosphate Receptors
Published on: June 8, 2022
Class II G protein-coupled receptors for VIP and PACAP: structure, models of activation and pharmacology
Marc Laburthe1, Alain Couvineau, Var Tan
1INSERM, U773, Centre de Recherche Biomédicale Bichat Beaujon, CRB3, Université Paris 7 Denis Diderot, BP416, F-75018 Paris, France. laburthe@bichat.inserm.fr
Abstract:
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.
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