1d0w
From Proteopedia
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|PDB= 1d0w |SIZE=350|CAPTION= <scene name='initialview01'>1d0w</scene> | |PDB= 1d0w |SIZE=350|CAPTION= <scene name='initialview01'>1d0w</scene> | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand=NH2:AMINO GROUP'>NH2</scene> | + | |LIGAND= <scene name='pdbligand=AYA:N-ACETYLALANINE'>AYA</scene>, <scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene> |
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1d0w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1d0w OCA], [http://www.ebi.ac.uk/pdbsum/1d0w PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1d0w RCSB]</span> | ||
}} | }} | ||
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[[Category: Norton, R S.]] | [[Category: Norton, R S.]] | ||
[[Category: Yao, S.]] | [[Category: Yao, S.]] | ||
| - | [[Category: NH2]] | ||
[[Category: helix]] | [[Category: helix]] | ||
[[Category: lactam-bridged]] | [[Category: lactam-bridged]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 19:32:17 2008'' |
Revision as of 16:32, 30 March 2008
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| Ligands: | , | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
SOLUTION STRUCTURE OF LACTAM-BRIDGED C-TERMINAL ANALOGUE-I 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
1D0W is a Protein complex structure of sequences from [1]. 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
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