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Molecular Pharmacology and Structure-Function Analysis of PACAP/Vip Receptors

  • Chapter
Pituitary Adenylate Cyclase-Activating Polypeptide

Part of the book series: Endocrine Updates ((ENDO,volume 20))

Abstract

PACAP (Arimura and Shioda, 1995; Vaudry et al, 2000) and VIP (Said, 1986; Laburthe et al, 1999) are two prominent neuropeptides which have wide distribution in peripheral and central nervous systems and large spectrum of biological actions. The 28-aminoacid peptide VIP was discovered in 1970 (Said and Mutt, 1970) and VIP receptors were shortly described in the seventies (Laburthe et al, 1993; for review). PACAP was isolated much later in 1989 (Miyata et al, 1989) as a 38-aminoacid peptide but a shorter form PACAP27 (Miyata et al, 1990) is also present in various tissues (Arimura and Shioda, 1995; Vaudry et al, 2000). The sequence of PACAP27 shows 68% identity with that of VIP in humans. Therefore, VIP and PACAP are the most closely related peptides in terms of structure and function in the so-called VIP-secretin family of structurally related peptides that comprises secretin, glucagon and glucagon-like peptides I and II, peptide histidine isoleucineamide (PHI), helodermin, growth hormone-releasing factor (GRF) and gastric inhibitory polypeptide (GIP) (Laburthe et al, 1993). Soon after the discovery of PACAP, it was shown that PACAP was able to bind with high affinity to the classical VIP receptors (Shivers et al, 1991) and also had a specific receptor for which VIP has a very low affinity (Buscail et al, 1990; Gottschall et al, 1990). The rapid development of receptor cloning in the nineties provided evidence for three receptor subtypes for PACAP: the so-called VPAC1, VPAC2 and PAC1 receptors (see below). In this context, the present chapter reviews the data regarding the molecular pharmacology and structure-function relationship of PACAP receptors including VPAC1, VPAC2 and PAC1 with special emphasis on receptors from humans and rats.

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Authors and Affiliations

  1. INSERM U410, Faculté de Médecine Xavier Bichat, Paris, 75018, France

    M. Laburthe, A. Couvineau & P. Nicole

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  1. M. Laburthe
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  2. A. Couvineau
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  3. P. Nicole
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  1. European Institute for Peptide Research, INSERM Unit 413, University of Rouen, Mont-Saint-Aignan, France

    Hubert Vaudry

  2. US Japan Biomedial Research Laboratories, Tulane University, Belle Chasse, Louisiana, USA

    Akira Arimura

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Laburthe, M., Couvineau, A., Nicole, P. (2003). Molecular Pharmacology and Structure-Function Analysis of PACAP/Vip Receptors. In: Vaudry, H., Arimura, A. (eds) Pituitary Adenylate Cyclase-Activating Polypeptide. Endocrine Updates, vol 20. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-0243-2_4

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