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Class II G protein-coupled receptors for VIP and PACAP: structure, models of activation and pharmacology.

Authors
Type
Published Article
Journal
JAMA Dermatology
Publisher
American Medical Association
Publication Date
September 2007
Volume
28
Issue
9
Pages
1631–1639
Identifiers
PMID: 17574305
Source
USPC - SET - SVS
License
Unknown

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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