PMID: 9437714Jan 1, 1997Paper

Development of high affinity selective VIP1 receptor agonists

Peptides
P GourletP Robberecht

Abstract

The biological effects of VIP are mediated by at least two VIP receptors: the VIP1 and the VIP2 receptors that were cloned in rat, human and mice. As the mRNA coding for each receptor are located in different tissues, it is likely that each receptor modulates different functions. It is therefore of interest to obtain selective agonists for each receptor subtype. In the present work, we achieved the synthesis of two VIP1 receptor selective agonsits derived from secretin and GRF. [R16]chicken secretin had IC50 values of binding of 1,10,000, 20, and 3000 nM for the rat VIP1-, VIP2-, secretion- and PACAP receptors, respectively. This peptide, however, had a weaker affinity for the human VIP1 receptor (IC50 of 60 nM). The chimeric, substituted peptide [K15, R16, L27]VIP(1-7)/GRF(8-27) had IC50 values of binding of 1,10,000, 10,000 and 30,000 nM for the rat VIP1-, VIP2-, secretin- and PACAP receptors, respectively. Furthermore, its also showed an IC50 of 0.8 nM for the human VIP1 receptor and a low affinity for the human VIP2 receptor. It is unlikely that this GRF analogue interacted with a high affinity to the pituitary GRF receptors as it did not stimulate rat pituitary adenylate cyclase activity. The two described analogues stimul...Continue Reading

References

Sep 1, 1979·Analytical Biochemistry·T M ChangW Y Chey
Apr 1, 1974·Analytical Biochemistry·Y SalomonM Rodbell
Dec 15, 1994·Regulatory Peptides·E CiccarelliP Robberecht
Mar 29, 1994·Proceedings of the National Academy of Sciences of the United States of America·N InagakiS Seino
Apr 1, 1996·Journal of Cellular Physiology·P VertongenP Robberecht
Jan 1, 1996·Advances in Neuroimmunology·P RobberechtM Svoboda
Dec 1, 1995·Neuropeptides·K KrempelsE Mezey

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Citations

Jan 4, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Satomi OnoueShizuo Yamada
Sep 3, 1998·European Journal of Pharmacology·P GourletP Robberecht
Nov 27, 1998·European Journal of Pharmacology·P RobberechtR A Lefebvre
Nov 26, 2002·Journal of Neuroimmunology·Xiuju JiangDoina Ganea
Oct 24, 1998·Trends in Pharmacological Sciences·T Dickinson, S M Fleetwood-Walker
Aug 4, 1999·Trends in Pharmacological Sciences·T Dickinson, S M Fleetwood-Walker
Sep 11, 2002·Regulatory Peptides·M Laburthe, A Couvineau
Feb 11, 2003·Peptides·Terry W MoodyRobert T Jensen
May 22, 2002·Cellular Signalling·Ingrid LangerMagali Waelbroeck
Aug 28, 1998·British Journal of Pharmacology·B Y De WinterP A Pelckmans
Feb 24, 2001·The European Journal of Neuroscience·H E ReedH D Piggins
Jul 6, 2000·European Journal of Biochemistry·M C Vandermeers-PiretP Robberecht
Feb 3, 1999·Annals of the New York Academy of Sciences·P Robberecht, M Waelbroeck
Feb 3, 1999·Annals of the New York Academy of Sciences·P VertongenP Robberecht
Nov 8, 2001·Proceedings of the National Academy of Sciences of the United States of America·E J GoetzlA J Harmar
Jul 17, 1999·The Journal of Peptide Research : Official Journal of the American Peptide Society·C EspositoM Cartenì-Farina
Aug 13, 2014·Journal of Molecular Neuroscience : MN·Tamás JuhászRóza Zákány

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