2h8s

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[[Image:2h8s.gif|left|200px]]
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[[Image:2h8s.png|left|200px]]
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{{STRUCTURE_2h8s| PDB=2h8s | SCENE= }}
{{STRUCTURE_2h8s| PDB=2h8s | SCENE= }}
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'''Solution structure of alpha-conotoxin Vc1.1'''
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===Solution structure of alpha-conotoxin Vc1.1===
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==Overview==
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The alpha-conotoxin Vc1.1 is a small disulfide-bonded peptide currently in development as a treatment for neuropathic pain. This study describes the synthesis, determination of the disulfide connectivity, and the determination of the three-dimensional structure of Vc1.1 using NMR spectroscopy. Vc1.1 was shown to inhibit nicotine-evoked membrane currents in isolated bovine chromaffin cells in a concentration-dependent manner and preferentially targets peripheral nicotinic acetylcholine receptor (nAChR) subtypes over central subtypes. Specifically, Vc1.1 is selective for alpha3-containing nAChR subtypes. The three-dimensional structure of Vc1.1 comprises a small alpha-helix spanning residues Pro6 to Asp11 and is braced by the I-III, II-IV disulfide connectivity seen in other alpha-conotoxins. A comparison of the structure of Vc1.1 with other alpha-conotoxins, taken together with nAChR selectivity data, suggests that the conserved proline at position 6 is important for binding, whereas a number of residues in the C-terminal portion of the peptide contribute toward the selectivity. The structure reported here should open new opportunities for further development of Vc1.1 or analogues as analgesic agents.
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(as it appears on PubMed at http://www.pubmed.gov), where 16754662 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16754662}}
==About this Structure==
==About this Structure==
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2H8S is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2H8S OCA].
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2H8S is a [[Single protein]] structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2H8S OCA].
==Reference==
==Reference==
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[[Category: Amidated c-terminus]]
[[Category: Amidated c-terminus]]
[[Category: Disulfide bond]]
[[Category: Disulfide bond]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:00:09 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 07:45:18 2008''

Revision as of 04:45, 28 July 2008

Template:STRUCTURE 2h8s

Solution structure of alpha-conotoxin Vc1.1

Template:ABSTRACT PUBMED 16754662

About this Structure

2H8S is a Single protein structure. Full experimental information is available from OCA.

Reference

The synthesis, structural characterization, and receptor specificity of the alpha-conotoxin Vc1.1., Clark RJ, Fischer H, Nevin ST, Adams DJ, Craik DJ, J Biol Chem. 2006 Aug 11;281(32):23254-63. Epub 2006 Jun 5. PMID:16754662

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