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  • Title: Hexanoylation of a VPAC2 receptor-preferring ligand markedly increased its selectivity and potency.
    Author: Langer I, Gregoire F, Nachtergael I, De Neef P, Vertongen P, Robberecht P.
    Journal: Peptides; 2004 Feb; 25(2):275-8. PubMed ID: 15063009.
    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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