6cmh
From Proteopedia
(New page: 200px<br /><applet load="6cmh" size="450" color="white" frame="true" align="right" spinBox="true" caption="6cmh" /> '''SYNTHETIC LINEAR MODIFIED ENDOTHELIN-1 AGONI...) |
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| - | [[Image:6cmh.gif|left|200px]]<br /><applet load="6cmh" size=" | + | [[Image:6cmh.gif|left|200px]]<br /><applet load="6cmh" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="6cmh" /> | caption="6cmh" /> | ||
'''SYNTHETIC LINEAR MODIFIED ENDOTHELIN-1 AGONIST'''<br /> | '''SYNTHETIC LINEAR MODIFIED ENDOTHELIN-1 AGONIST'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The solution structure of a biologically active modified linear | + | The solution structure of a biologically active modified linear endothelin-1 analogue, ET1-21[Cys(Acm)1,15, Aib3,11, Leu7], has been determined for the first time by two-dimensional nuclear magnetic resonance spectroscopy in a methanol-d3/water solvent mixture. Out of approximately one hundred linear peptide analogues tested by biological assay, this peptide, together with a dozen others, showed significant ETB selective agonist activity. Here we report the solution structure of an ETB selective agonist of a full-length, synthetic linear endothelin analogue. The calculated structures indicate that the peptide adopts an alpha-helical conformation between residues Ser5-His16, whilst both N- and C-termini show no preferred conformation. These results suggest that the disulphide bridges normally associated with endothelin and sarafotoxin peptides may not necessarily be important for either ETB receptor binding activity or the formation of a helical conformation in solution. |
==About this Structure== | ==About this Structure== | ||
| - | 6CMH is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/ ]. Full crystallographic information is available from [http:// | + | 6CMH is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/ ]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6CMH OCA]. |
==Reference== | ==Reference== | ||
Solution structure of a novel ETB receptor selective agonist ET1-21 [Cys(Acm)1,15, Aib3,11, Leu7] by nuclear magnetic resonance spectroscopy and molecular modelling., Hewage CM, Jiang L, Parkinson JA, Ramage R, Sadler IH, J Pept Res. 1999 Mar;53(3):223-33. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=10231710 10231710] | Solution structure of a novel ETB receptor selective agonist ET1-21 [Cys(Acm)1,15, Aib3,11, Leu7] by nuclear magnetic resonance spectroscopy and molecular modelling., Hewage CM, Jiang L, Parkinson JA, Ramage R, Sadler IH, J Pept Res. 1999 Mar;53(3):223-33. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=10231710 10231710] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Hewage, C | + | [[Category: Hewage, C M.]] |
[[Category: Jiang, L.]] | [[Category: Jiang, L.]] | ||
| - | [[Category: Parkinson, J | + | [[Category: Parkinson, J A.]] |
[[Category: Ramage, R.]] | [[Category: Ramage, R.]] | ||
| - | [[Category: Sadler, I | + | [[Category: Sadler, I H.]] |
[[Category: endothelin-1]] | [[Category: endothelin-1]] | ||
[[Category: vasoconstrictor]] | [[Category: vasoconstrictor]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 19:16:14 2008'' |
Revision as of 17:16, 21 February 2008
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SYNTHETIC LINEAR MODIFIED ENDOTHELIN-1 AGONIST
Overview
The solution structure of a biologically active modified linear endothelin-1 analogue, ET1-21[Cys(Acm)1,15, Aib3,11, Leu7], has been determined for the first time by two-dimensional nuclear magnetic resonance spectroscopy in a methanol-d3/water solvent mixture. Out of approximately one hundred linear peptide analogues tested by biological assay, this peptide, together with a dozen others, showed significant ETB selective agonist activity. Here we report the solution structure of an ETB selective agonist of a full-length, synthetic linear endothelin analogue. The calculated structures indicate that the peptide adopts an alpha-helical conformation between residues Ser5-His16, whilst both N- and C-termini show no preferred conformation. These results suggest that the disulphide bridges normally associated with endothelin and sarafotoxin peptides may not necessarily be important for either ETB receptor binding activity or the formation of a helical conformation in solution.
About this Structure
6CMH is a Single protein structure of sequence from [1]. Full crystallographic information is available from OCA.
Reference
Solution structure of a novel ETB receptor selective agonist ET1-21 [Cys(Acm)1,15, Aib3,11, Leu7] by nuclear magnetic resonance spectroscopy and molecular modelling., Hewage CM, Jiang L, Parkinson JA, Ramage R, Sadler IH, J Pept Res. 1999 Mar;53(3):223-33. PMID:10231710
Page seeded by OCA on Thu Feb 21 19:16:14 2008
