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| - | [[Image:1tr6.jpg|left|200px]] | + | {{Seed}} |
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| | {{STRUCTURE_1tr6| PDB=1tr6 | SCENE= }} | | {{STRUCTURE_1tr6| PDB=1tr6 | SCENE= }} |
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| - | '''NMR solution structure of omega-conotoxin [K10]GVIA, a cyclic cysteine knot peptide'''
| + | ===NMR solution structure of omega-conotoxin [K10]GVIA, a cyclic cysteine knot peptide=== |
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| - | ==Overview==
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| - | The omega-conotoxins from fish-hunting cone snails are potent inhibitors of voltage-gated calcium channels. The omega-conotoxins MVIIA and CVID are selective N-type calcium channel inhibitors with potential in the treatment of chronic pain. The beta and alpha(2)delta-1 auxiliary subunits influence the expression and characteristics of the alpha(1B) subunit of N-type channels and are differentially regulated in disease states, including pain. In this study, we examined the influence of these auxiliary subunits on the ability of the omega-conotoxins GVIA, MVIIA, CVID and analogues to inhibit peripheral and central forms of the rat N-type channels. Although the beta3 subunit had little influence on the on- and off-rates of omega-conotoxins, coexpression of alpha(2)delta with alpha(1B) significantly reduced on-rates and equilibrium inhibition at both the central and peripheral isoforms of the N-type channels. The alpha(2)delta also enhanced the selectivity of MVIIA, but not CVID, for the central isoform. Similar but less pronounced trends were also observed for N-type channels expressed in human embryonic kidney cells. The influence of alpha(2)delta was not affected by oocyte deglycosylation. The extent of recovery from the omega-conotoxin block was least for GVIA, intermediate for MVIIA, and almost complete for CVID. Application of a hyperpolarizing holding potential (-120 mV) did not significantly enhance the extent of CVID recovery. Interestingly, [R10K]MVIIA and [O10K]GVIA had greater recovery from the block, whereas [K10R]CVID had reduced recovery from the block, indicating that position 10 had an important influence on the extent of omega-conotoxin reversibility. Recovery from CVID block was reduced in the presence of alpha(2)delta in human embryonic kidney cells and in oocytes expressing alpha(1B-b). These results may have implications for the antinociceptive properties of omega-conotoxins, given that the alpha(2)delta subunit is up-regulated in certain pain states.
| + | The line below this paragraph, {{ABSTRACT_PUBMED_15166237}}, adds the Publication Abstract to the page |
| | + | (as it appears on PubMed at http://www.pubmed.gov), where 15166237 is the PubMed ID number. |
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| | + | {{ABSTRACT_PUBMED_15166237}} |
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| | ==About this Structure== | | ==About this Structure== |
| - | 1TR6 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Conus_geographus Conus geographus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1TR6 OCA]. | + | 1TR6 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Conus_geographus Conus geographus]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1TR6 OCA]. |
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| | ==Reference== | | ==Reference== |
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| | [[Category: Cysteine knot]] | | [[Category: Cysteine knot]] |
| | [[Category: Four-loop frame work]] | | [[Category: Four-loop frame work]] |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 10:16:39 2008'' | + | |
| | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:08:17 2008'' |
Revision as of 13:08, 28 July 2008
Template:STRUCTURE 1tr6
NMR solution structure of omega-conotoxin [K10]GVIA, a cyclic cysteine knot peptide
Template:ABSTRACT PUBMED 15166237
About this Structure
1TR6 is a Single protein structure of sequence from Conus geographus. Full experimental information is available from OCA.
Reference
The alpha2delta auxiliary subunit reduces affinity of omega-conotoxins for recombinant N-type (Cav2.2) calcium channels., Mould J, Yasuda T, Schroeder CI, Beedle AM, Doering CJ, Zamponi GW, Adams DJ, Lewis RJ, J Biol Chem. 2004 Aug 13;279(33):34705-14. Epub 2004 May 27. PMID:15166237
Page seeded by OCA on Mon Jul 28 16:08:17 2008
