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VPAC and PAC receptors: From ligands to function.

Louise Dickson¹, Keith Finlayson

¹Centre for Integrative Physiology, University of Edinburgh, EH8 9XD, UK.

Pharmacology & Therapeutics

|December 27, 2008

Summary

Vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase activating polypeptides (PACAPs) are key signaling molecules. Despite extensive research, a lack of selective non-peptide ligands hinders understanding of their roles and therapeutic potential.

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Area of Science:

Neuroendocrinology
Molecular Pharmacology
Gastroenterology

Background:

Vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase activating polypeptides (PACAPs) are related secretin family peptides with diverse physiological roles.
These peptides signal through three common G-protein coupled receptors: VPAC1, VPAC2, and PAC1R, primarily activating adenylate cyclase and increasing intracellular cAMP.
VIP and PACAP actions are implicated in numerous processes, including circadian rhythms and diseases like pulmonary hypertension, making them pharmaceutical targets.

Purpose of the Study:

To review current knowledge on VIP/PACAP peptides and their receptors (VPAC1, VPAC2, PAC1R).
To highlight the distribution, pharmacology, signaling pathways, and splice variants of these receptors.
To discuss the utility of animal models in understanding the physiological roles of VIP/PACAP signaling.

Main Methods:

Review of existing literature on VIP, PACAP, and their receptors.
Analysis of data from in vitro cell-based functional assays.
Examination of findings from transgenic animal models and rodent disease models.

Main Results:

VIP and PACAP share significant amino acid identity and activate common G-protein coupled receptors.
Receptor activation influences various physiological processes and clinical conditions.
A significant limitation in the field is the scarcity of selective, non-peptide ligands for these receptors.

Conclusions:

VIP/PACAP peptides and their receptors are crucial in diverse physiological functions and disease states.
Further research into selective ligands is essential for advancing basic understanding and therapeutic applications.
Animal models provide valuable insights into the complex roles of the VIP/PACAP system.