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1d1e
From Proteopedia
(New page: 200px<br /><applet load="1d1e" size="450" color="white" frame="true" align="right" spinBox="true" caption="1d1e" /> '''SOLUTION STRUCTURE OF LACTAM-BRIDGED C-TERMI...) |
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'''SOLUTION STRUCTURE OF LACTAM-BRIDGED C-TERMINAL ANALOGUE-II OF NEUROPEPTIDE Y'''<br /> | '''SOLUTION STRUCTURE OF LACTAM-BRIDGED C-TERMINAL ANALOGUE-II OF NEUROPEPTIDE Y'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The importance of helical structure in an analogue of NPY selective for | + | 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. |
==About this Structure== | ==About this Structure== | ||
| - | 1D1E is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/ ] with ACE and NH2 as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1D1E is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/ ] with <scene name='pdbligand=ACE:'>ACE</scene> and <scene name='pdbligand=NH2:'>NH2</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1D1E OCA]. |
==Reference== | ==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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12014969 12014969] | 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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12014969 12014969] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| - | [[Category: Norton, R | + | [[Category: Norton, R S.]] |
[[Category: Yao, S.]] | [[Category: Yao, S.]] | ||
[[Category: ACE]] | [[Category: ACE]] | ||
| Line 19: | Line 19: | ||
[[Category: lactam-bridge]] | [[Category: lactam-bridge]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:11:55 2008'' |
Revision as of 10:12, 21 February 2008
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SOLUTION STRUCTURE OF LACTAM-BRIDGED C-TERMINAL ANALOGUE-II OF NEUROPEPTIDE Y
Overview
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.
About this Structure
1D1E is a Protein complex structure of sequences from [1] with and as ligands. Full crystallographic 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 Thu Feb 21 12:11:55 2008
Categories: Protein complex | Norton, R S. | Yao, S. | ACE | NH2 | Helix | Lactam-bridge
