Literature DB >> 9650836

Vasoactive intestinal peptide modification at position 22 allows discrimination between receptor subtypes.

P Gourlet1, M C Vandermeers-Piret, J Rathé, P De Neef, J Cnudde, P Robberecht, M Waelbroeck.   

Abstract

Secretin and growth hormone releasing factor (GRF) have a weak affinity for VIP (vasoactive intestinal peptide)/PACAP (pituitary adenylate cyclase activating polypeptide) receptors, but discriminate between VIP1/PACAP and VIP2/PACAP receptors. This previously allowed us to develop modified secretin and GRF derivatives as high affinity and highly selective VIP1/PACAP receptor ligands. We tested the hypothesis that the presence of a Gln residue at position 24 and a Leu residue at position 22 was responsible for their VIP1/PACAP receptor selectivity. [Gln24]VIP was not different from VIP but [Leu22]VIP had a 100-fold lower affinity for VIP2/PACAP receptors as compared to VIP1/PACAP receptors. The substitution of Tyr22 by Phe22 in VIP had no significant effect on the recognition of both receptors but [Ala22]VIP had a reduced affinity for the VIP2/PACAP receptor. This indicated that an aromatic residue at position 22 of VIP was required for a high affinity for the VIP2/PACAP receptor but not for the VIP1/PACAP receptor.

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Year:  1998        PMID： 9650836     DOI： 10.1016/s0014-2999(98)00133-2

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  11 in total

1.  (N-stearyl, norleucine17)VIPhybrid is a broad spectrum vasoactive intestinal peptide receptor antagonist.

Authors:  Terry W Moody; Robert T Jensen; Mati Fridkin; Illana Gozes
Journal:  J Mol Neurosci       Date:  2002 Feb-Apr       Impact factor: 3.444

2.  Antagonistic actions of analogs related to growth hormone-releasing hormone (GHRH) on receptors for GHRH and vasoactive intestinal peptide on rat pituitary and pineal cells in vitro.

Authors:  Z Rekasi; J L Varga; A V Schally; G Halmos; K Groot; T Czompoly
Journal:  Proc Natl Acad Sci U S A       Date:  2000-02-01       Impact factor: 11.205

3.  Two tyrosine residues in the first transmembrane helix of the human vasoactive intestinal peptide receptors play a role in supporting the active conformation.

Authors:  J Perret; P Vertongen; R M Solano; I Langer; J Cnudde; P Robberecht; M Waelbroeck
Journal:  Br J Pharmacol       Date:  2002-08       Impact factor: 8.739

4.  Evidence for a direct interaction between the Thr11 residue of vasoactive intestinal polypeptide and Tyr184 located in the first extracellular loop of the VPAC2 receptor.

Authors:  Ingrid Nachtergael; Pascale Vertongen; Ingrid Langer; Jason Perret; Patrick Robberecht; Magali Waelbroeck
Journal:  Biochem J       Date:  2003-03-15       Impact factor: 3.857

5.  Receptors for VIP and PACAP in guinea pig cerebral cortex: effects on cyclic AMP synthesis and characterization by 125I-VIP binding.

Authors:  Jolanta B Zawilska; Agnieszka Dejda; Pawel Niewiadomski; Illana Gozes; Jerzy Z Nowak
Journal:  J Mol Neurosci       Date:  2005       Impact factor: 3.444

6.  A structure-function study of PACAP using conformationally restricted analogs: Identification of PAC1 receptor-selective PACAP agonists.

Authors:  Irene Ramos-Álvarez; Samuel A Mantey; Taichi Nakamura; Bernardo Nuche-Berenguer; Paola Moreno; Terry W Moody; Jerome L Maderdrut; David H Coy; Robert T Jensen
Journal:  Peptides       Date:  2015-02-16       Impact factor: 3.750

7.  Characterization of a novel VPAC(1) selective agonist and identification of the receptor domains implicated in the carboxyl-terminal peptide recognition.

Authors:  J Van Rampelbergh; M G Juarranz; J Perret; A Bondue; R M Solano; C Delporte; P De Neef; P Robberecht; M Waelbroeck
Journal:  Br J Pharmacol       Date:  2000-06       Impact factor: 8.739

Review 8.  Targeting the PAC1 Receptor for Neurological and Metabolic Disorders.

Authors:  Chenyi Liao; Mathilde P de Molliens; Severin T Schneebeli; Matthias Brewer; Gaojie Song; David Chatenet; Karen M Braas; Victor May; Jianing Li
Journal:  Curr Top Med Chem       Date:  2019       Impact factor: 3.295

9.  Agnathan VIP, PACAP and their receptors: ancestral origins of today's highly diversified forms.

Authors:  Stephanie Y L Ng; Billy K C Chow; Jun Kasamatsu; Masanori Kasahara; Leo T O Lee
Journal:  PLoS One       Date:  2012-09-05       Impact factor: 3.240

Review 10.  A Clinical Approach for the Use of VIP Axis in Inflammatory and Autoimmune Diseases.

Authors:  Carmen Martínez; Yasmina Juarranz; Irene Gutiérrez-Cañas; Mar Carrión; Selene Pérez-García; Raúl Villanueva-Romero; David Castro; Amalia Lamana; Mario Mellado; Isidoro González-Álvaro; Rosa P Gomariz
Journal:  Int J Mol Sci       Date:  2019-12-20       Impact factor: 5.923
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