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

European Journal of Pharmacology
P GourletM 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.

References

Mar 1, 1989·Biological Chemistry Hoppe-Seyler·D AmbrosiusH Zahn
Apr 1, 1974·Analytical Biochemistry·Y SalomonM Rodbell
Dec 15, 1994·Regulatory Peptides·E CiccarelliP Robberecht
Dec 30, 1994·Biochemical and Biophysical Research Communications·M SvobodaP Robberecht
Mar 29, 1994·Proceedings of the National Academy of Sciences of the United States of America·N InagakiS Seino
Apr 29, 1994·Biochemical and Biophysical Research Communications·A CouvineauM Laburthe
Jan 1, 1996·Advances in Neuroimmunology·P RobberechtM Svoboda
Oct 1, 1996·International Journal of Peptide and Protein Research·P GourletP Robberecht
Jan 1, 1997·Peptides·P GourletP Robberecht
Feb 3, 1999·Annals of the New York Academy of Sciences·P GourletP Robberecht

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Citations

Sep 11, 2002·Regulatory Peptides·M Laburthe, A Couvineau
Feb 11, 2003·Peptides·Terry W MoodyRobert T Jensen
Sep 12, 2006·Regulatory Peptides·David DangoorIllana Gozes
Dec 22, 2019·International Journal of Molecular Sciences·Carmen MartínezRosa P Gomariz
Jan 25, 2000·American Journal of Physiology. Gastrointestinal and Liver Physiology·T ItoR T Jensen
Jul 10, 2019·Current Topics in Medicinal Chemistry·Chenyi LiaoJianing Li

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