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'''SOLUTION STRUCTURE OF LACTAM-BRIDGED C-TERMINAL ANALOGUE-I OF NEUROPEPTIDE Y''' | '''SOLUTION STRUCTURE OF LACTAM-BRIDGED C-TERMINAL ANALOGUE-I OF NEUROPEPTIDE Y''' | ||
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==About this Structure== | ==About this Structure== | ||
Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1D0W 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://www.ncbi.nlm.nih.gov/pubmed/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://www.ncbi.nlm.nih.gov/pubmed/12014969 12014969] | ||
[[Category: Norton, R S.]] | [[Category: Norton, R S.]] | ||
[[Category: Yao, S.]] | [[Category: Yao, S.]] | ||
[[Category: | [[Category: Helix]] | ||
[[Category: | [[Category: Lactam-bridged]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 13:19:30 2008'' | |||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | |||
Revision as of 10:19, 2 May 2008
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
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 Fri May 2 13:19:30 2008
