1fvn
From Proteopedia
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[[Image:1fvn.gif|left|200px]] | [[Image:1fvn.gif|left|200px]] | ||
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'''[ALA31, AIB32]-NEUROPEPTIDE Y''' | '''[ALA31, AIB32]-NEUROPEPTIDE Y''' | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1FVN is a [[Single protein]] structure | + | 1FVN is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1FVN OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Zerbe, O.]] | [[Category: Zerbe, O.]] | ||
[[Category: 310-helix]] | [[Category: 310-helix]] | ||
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| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 16:48:52 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 13:48, 2 May 2008
[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. 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 Page seeded by OCA on Fri May 2 16:48:52 2008
