1fvn

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[ALA31, AIB32]-NEUROPEPTIDE Y

Overview

The first Y(5) receptor-selective analog of neuropeptide Y (NPY), [Ala(31),Aib(32)]NPY, has been developed and biologically characterized., Using competition binding assays on cell lines that express different Y, receptors, we determined the affinity of this analog to be 6 nm at the, human Y(5) receptor, >500 nm at the Y(1) and Y(2) receptors, and >1000 nm, at the Y(4) receptor. Activity studies performed in vitro using a cAMP, enzyme immunoassay, and in vivo using food intake studies in rats, showed, that the peptide acted as an agonist. Further peptides obtained by the, combination of the Ala(31)-Aib(32) motif with chimeric peptides containing, segments of NPY and pancreatic polypeptide displayed the same selectivity, and even higher affinity (up to 0.2 nm) for the Y(5) receptor. In vivo, administration of the new Y(5) receptor-selective agonists significantly, stimulated feeding in rats. The NMR solution structures of NPY and, [Ala(31),Aib(32)]NPY showed a different conformation in the C-terminal, region, where the alpha-helix of NPY was substituted by a more flexible, 3(10)-helical turn structure.

About this Structure

1FVN is a Single protein structure of sequence from [1] with NH2 as ligand. Full crystallographic information is available from OCA.

Reference

The first selective agonist for the neuropeptide YY5 receptor increases food intake in rats., Cabrele C, Langer M, Bader R, Wieland HA, Doods HN, Zerbe O, Beck-Sickinger AG, J Biol Chem. 2000 Nov 17;275(46):36043-8. PMID:10944518

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