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| [[Image:2h8s.gif|left|200px]] | | {{Seed}} |
| | [[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'''
| | ===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. | | The line below this paragraph, {{ABSTRACT_PUBMED_16754662}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 16754662 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_16754662}} |
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| ==About this Structure== | | ==About this Structure== |
| 2H8S is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2H8S OCA]. | | 2H8S is a [[Single protein]] structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2H8S OCA]. |
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| ==Reference== | | ==Reference== |
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| [[Category: Amidated c-terminus]] | | [[Category: Amidated c-terminus]] |
| [[Category: Disulfide bond]] | | [[Category: Disulfide bond]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:00:09 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 07:45:18 2008'' |
