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1d0w

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{{STRUCTURE_1d0w| PDB=1d0w | SCENE= }}
{{STRUCTURE_1d0w| PDB=1d0w | SCENE= }}
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'''SOLUTION STRUCTURE OF LACTAM-BRIDGED C-TERMINAL ANALOGUE-I OF NEUROPEPTIDE Y'''
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===SOLUTION STRUCTURE OF LACTAM-BRIDGED C-TERMINAL ANALOGUE-I OF NEUROPEPTIDE Y===
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==Overview==
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The importance of helical structure in an analogue of NPY selective for the Y2 receptor, Ac[Leu28,31]NPY24-36, has been investigated by introducing a lactam bridge between positions 28 and 32. The resulting analogue, Ac-cyclo28/32[Ala24,Lys28,Leu31,Glu32]NPY24-36, is a potent Y2-selective agonist. Structural analysis by NMR shows that this analogue forms a helical structure in a 40% trifluoroethanol/water mixture, whereas in water only the region around the lactam bridge (Lys28-Glu32) adopts helical-like structure, with both N- and C-termini being poorly defined. The observation of well-defined helical structure in aqueous TFE contrasts with that reported for a similar analogue, Ac-cyclo28/32[Lys28,Glu32]NPY25-36 (Rist et al. FEBS Lett. 1996, 394, 169-173), which consisted of a hairpin-like structure that brought the N- and C-termini into proximity. We have therefore determined the structures of this analogue, as well as those of Ac-cyclo28/32[Ala24,Lys28,Leu31,Glu32]NPY24-36 and Ac-cyclo28/32[Ala24,Lys28,Glu32]NPY24-36, under identical solution conditions (30% TFE/H2O mixture at 308 K) and find essentially the same helical structure in all three peptides. These findings support the proposal that these Y2-selective analogues adopt a helical structure when bound to the Y2 receptor.
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(as it appears on PubMed at http://www.pubmed.gov), where 12014969 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12014969}}
==About this Structure==
==About this Structure==
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Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1D0W OCA].
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Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1D0W OCA].
==Reference==
==Reference==
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[[Category: Helix]]
[[Category: Helix]]
[[Category: Lactam-bridged]]
[[Category: Lactam-bridged]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 13:19:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 21:58:51 2008''

Revision as of 18:59, 30 June 2008

Image:1d0w.png

Template:STRUCTURE 1d0w

SOLUTION STRUCTURE OF LACTAM-BRIDGED C-TERMINAL ANALOGUE-I OF NEUROPEPTIDE Y

Template:ABSTRACT PUBMED 12014969

About this Structure

Full experimental information is available from OCA.

Reference

Stabilization of the helical structure of Y2-selective analogues of neuropeptide Y by lactam bridges., Yao S, Smith-White MA, Potter EK, Norton RS, J Med Chem. 2002 May 23;45(11):2310-8. PMID:12014969

Page seeded by OCA on Mon Jun 30 21:58:51 2008

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