Development of High Affinity Selective VIP1 Receptor Agonists

Gourlet, Philippe; Vandermeers, André; Vertongen, Pascale; Rathé, Jean; Neef, Philippe De; Cnudde, Johnny; Waelbroeck, Magalì; Robberecht, Patrick

doi:10.1016/s0196-9781(97)00228-3

Cited by 181 publications

(124 citation statements)

References 30 publications

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“…To evaluate the functionality of the VIP receptors expressed in skeletal muscle and to validate the observation that only VPAC2R is expressed in skeletal muscle, skeletal muscles in organ bath were stimulated with either the VPACR-nonselective agonist VIP, the VPAC1R-selective agonist [K 15 ,R (8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27), or the VPAC2R-selective agonist Ro-25-1553, and cAMP generation was evaluated. As can be seen in Fig.…”

Section: Resultsmentioning

confidence: 99%

Activation of the vasoactive intestinal peptide 2 receptor modulates normal and atrophying skeletal muscle mass and force

Hinkle¹,

Donnelly²,

Cody³

et al. 2005

Journal of Applied Physiology

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Section: Resultsmentioning

confidence: 99%

Activation of the vasoactive intestinal peptide 2 receptor modulates normal and atrophying skeletal muscle mass and force

Hinkle¹,

Donnelly²,

Cody³

et al. 2005

Journal of Applied Physiology

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“…7). Two VPAC 1 receptor selective agonists derived from secretin and GRF were previously described (59,60). Chicken [Arg 16 ]secretin, although it discriminates between rat VPAC 1 and VPAC 2 receptors, has a high affinity for rat secretin receptor (59).…”

Section: Discussionmentioning

confidence: 99%

“…Two VPAC 1 receptor selective agonists derived from secretin and GRF were previously described (59,60). Chicken [Arg 16 ]secretin, although it discriminates between rat VPAC 1 and VPAC 2 receptors, has a high affinity for rat secretin receptor (59). Moreover, it has a rather weak affinity for the human VPAC 1 receptor (60), in line with the important differences between species in the pharmacology of VPAC 1 receptors (15,44 ]VIP (1-7)/GRF (8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27) has an important selectivity for VPAC 1 receptor but its possible interaction with GRF receptors was not directly evaluated (61).…”

Section: Discussionmentioning

confidence: 99%

Identification of Key Residues for Interaction of Vasoactive Intestinal Peptide with Human VPAC1 and VPAC2Receptors and Development of a Highly Selective VPAC1Receptor Agonist

Nicole

Lins

Rouyer‐Fessard

et al. 2000

Journal of Biological Chemistry

158

161

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The widespread neuropeptide vasoactive intestinal peptide (VIP) has two receptors VPAC 1 and VPAC 2 . Solid-phase syntheses of VIP analogs in which each amino acid has been changed to alanine (Ala scan) or glycine was achieved and each analog was tested for: (i) threedimensional structure by ab initio molecular modeling; (ii) ability to inhibit 125 ]VIP analog which constitutes the first highly selective (>1,000-fold) human VPAC 1 receptor agonist derived from VIP ever described. The vasoactive intestinal peptide (VIP)1 is a prominent neuropeptide with wide distribution in both peripheral and central nervous systems and a large spectrum of biological actions in mammals (1, 2). VIP-containing nerves and VIP effects have been described in digestive tract, cardiovascular system, airways, reproductive system, immune system, endocrine glands, and brain (1). Besides its short-term actions on exocrine secretions, hormone release, muscle relaxation, and metabolism (1, 2), VIP has been also characterized as a growth regulator for fetuses and tumor cells and during embryonic brain development (3). There are recent evidences for an important role of VIP in the perception of pain (4) and suppression of inflammation (5). Finally, VIP has been involved in diseases such as the watery diarrhea syndrome and clinical applications of VIP have been already suggested in impotence, asthma, lung injury, a variety of tumors and neurodegenerative diseases (1-3).VIP belongs to a large family of structurally related peptides (2, 6, 7) that comprises VIP, pituitary adenylate cyclase-activating peptide PACAP-27, and its C-terminal extended form PACAP-38, secretin, glucagon, and glucagon-like peptides-1 and -2, gastric inhibitory polypeptide, peptide histidine methionine amide, growth hormone-releasing factor (GRF), and peptides isolated from the venom of the Gila Monster. VIP and PACAP are the most closely related peptides in terms of structure and function (2, 6). They share two common receptors, VPAC 1 and VPAC 2 , which display high affinity for both VIP and PACAP (2,8). These receptors together with receptors for VIP-related peptides (see above) clearly constitute an original subfamily within the superfamily of G protein-coupled receptors (2, 9, 10). This subfamily referred to as class II (2) also comprises receptors for parathyroid hormone, calcitonin, corticotropin-releasing factor, and the so called EGF-TM7 receptors (11). Class II family of receptors for peptides display several common properties including large N-terminal extracellular domains containing highly conserved cystein residues, N-terminal leader sequences, and complex gene organization with many introns (2).Although the structure-function relationship of VIP receptors, including VPAC 1 and VPAC 2 , has been recently documented (2,9,(12)(13)(14)(15)(16)(17)(18)(19)(20), the structure-function relationship of VIP itself is still poorly understood. Some old studies carried out before the characterization and cloning of VIP receptor subtypes (21-23) indicated that: (i) th...

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“…(14,15) were added, incubations continued for 20 min at 37°C, and T cells were pelleted by centrifugation at 4°C for 10 min at 400 ϫ g. Results of preliminary studies at 2, 20, and 60 min showed maximal levels of cAMP at 20 min. After removal of supernates, the T cells were disrupted by incubation for 10 min at 37°C in 0.25 ml per well of 0.1 M HCl with 1% (v/v) Triton X-100 and re-centrifuged at 4°C for 10 min at 1,200 ϫ g. The [cAMP] i in the lysate supernates was quantified directly after acetylation with the Correlate-EIA kit (Assay Designs, Inc., Ann Arbor, MI); sensitivity ϭ 0.035 nM and mean recovery ϭ 85%.…”

Section: Identification Cloning and Sequencing Of Cdnas Encoding Mousementioning

confidence: 99%

A Natural Variant Type II G Protein-coupled Receptor for Vasoactive Intestinal Peptide with Altered Function

Grinninger¹,

Wang²,

Oskoui

et al. 2004

Journal of Biological Chemistry

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Development of High Affinity Selective VIP1 Receptor Agonists

Cited by 181 publications

References 30 publications

Activation of the vasoactive intestinal peptide 2 receptor modulates normal and atrophying skeletal muscle mass and force

Activation of the vasoactive intestinal peptide 2 receptor modulates normal and atrophying skeletal muscle mass and force

Identification of Key Residues for Interaction of Vasoactive Intestinal Peptide with Human VPAC1 and VPAC2Receptors and Development of a Highly Selective VPAC1Receptor Agonist

A Natural Variant Type II G Protein-coupled Receptor for Vasoactive Intestinal Peptide with Altered Function

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