1FVN

[ALA31, AIB32]-NEUROPEPTIDE Y

Summary for 1FVN

• Entry DOI: 10.2210/pdb1fvn/pdb
• Related: 1RON
• NMR Information: BMRB: 4862
• Descriptor: NEUROPEPTIDE Y (1 entity in total)
• Functional Keywords: alpha, 310-helix, hormone-growth factor complex, hormone/growth factor
• Total number of polymer chains: 1
• Total formula weight: 4200.61

Authors

Bader, R.,Zerbe, O.,Beck-Sickinger, A.G. (deposition date: 2000-09-20, release date: 2000-10-04, Last modification date: 2021-11-03)

Primary citation

Cabrele, C.,Langer, M.,Bader, R.,Wieland, H.A.,Doods, H.N.,Zerbe, O.,Beck-Sickinger, A.G.
The first selective agonist for the neuropeptide YY5 receptor increases food intake in rats.
J.Biol.Chem., 275:36043-36048, 2000

PubMed Abstract: 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.

PubMed: 10944518
DOI: 10.1074/jbc.M000626200

Experimental method

SOLUTION NMR