Literature DB >> 15063009

Hexanoylation of a VPAC2 receptor-preferring ligand markedly increased its selectivity and potency.

Ingrid Langer1, Françoise Gregoire, Ingrid Nachtergael, Philippe De Neef, Pascale Vertongen, Patrick Robberecht.   

Abstract

We synthesized a VIP analog that combines mutations that decrease the affinity for the VPAC1 receptor but maintain a high affinity for the VPAC2 receptor with an amino-terminal hexanoylation that increases the affinity for the VPAC2 receptor with a limited decrease in the affinity of the VPAC1 receptor. The resulting Hexanoyl[A19,K(27,28)]VIP had the expected properties of a high affinity for the VPAC2 receptor and a low affinity for the VPAC1 receptor and also a low affinity for the PAC1 and secretin receptors. With a 1000-fold preference for the VPAC2 receptor and a IC50 value of binding of 1 nM, this compound is the most potent and the most selective agonist presently described.

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Year:  2004        PMID： 15063009     DOI： 10.1016/j.peptides.2003.12.013

Source DB:  PubMed          Journal:  Peptides        ISSN： 0196-9781            Impact factor:   3.750


  4 in total

Review 1.  Structure and mechanism for recognition of peptide hormones by Class B G-protein-coupled receptors.

Authors:  Kuntal Pal; Karsten Melcher; H Eric Xu
Journal:  Acta Pharmacol Sin       Date:  2012-01-23       Impact factor: 6.150

Review 2.  Chemical modification of class II G protein-coupled receptor ligands: frontiers in the development of peptide analogs as neuroendocrine pharmacological therapies.

Authors:  Megan C Chapter; Caitlin M White; Angela DeRidder; Wayne Chadwick; Bronwen Martin; Stuart Maudsley
Journal:  Pharmacol Ther       Date:  2009-08-15       Impact factor: 12.310

3.  VIP blockade leads to microcephaly in mice via disruption of Mcph1-Chk1 signaling.

Authors:  Sandrine Passemard; Vincent El Ghouzzi; Hala Nasser; Catherine Verney; Guilan Vodjdani; Adrien Lacaud; Sophie Lebon; Marc Laburthe; Patrick Robberecht; Jeannette Nardelli; Shyamala Mani; Alain Verloes; Pierre Gressens; Vincent Lelièvre
Journal:  J Clin Invest       Date:  2011-08       Impact factor: 14.808

4.  Pituitary adenylate cyclase-activating polypeptide stimulates glucose production via the hepatic sympathetic innervation in rats.

Authors:  Chun-Xia Yi; Ning Sun; Mariette T Ackermans; Anneke Alkemade; Ewout Foppen; Jing Shi; Mireille J Serlie; Ruud M Buijs; Eric Fliers; Andries Kalsbeek
Journal:  Diabetes       Date:  2010-03-31       Impact factor: 9.461
  4 in total

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