1cnn: Difference between revisions
No edit summary |
No edit summary |
||
| Line 1: | Line 1: | ||
[[Image:1cnn.gif|left|200px]] | [[Image:1cnn.gif|left|200px]] | ||
'''OMEGA-CONOTOXIN MVIIC FROM CONUS MAGUS''' | {{Structure | ||
|PDB= 1cnn |SIZE=350|CAPTION= <scene name='initialview01'>1cnn</scene> | |||
|SITE= | |||
|LIGAND= <scene name='pdbligand=NH2:AMINO GROUP'>NH2</scene> | |||
|ACTIVITY= | |||
|GENE= | |||
}} | |||
'''OMEGA-CONOTOXIN MVIIC FROM CONUS MAGUS''' | |||
==Overview== | ==Overview== | ||
| Line 7: | Line 16: | ||
==About this Structure== | ==About this Structure== | ||
1CNN is a [ | 1CNN is a [[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=1CNN OCA]. | ||
==Reference== | ==Reference== | ||
Structure-activity relationships of omega-conotoxins MVIIA, MVIIC and 14 loop splice hybrids at N and P/Q-type calcium channels., Nielsen KJ, Adams D, Thomas L, Bond T, Alewood PF, Craik DJ, Lewis RJ, J Mol Biol. 1999 Jun 25;289(5):1405-21. PMID:[http:// | Structure-activity relationships of omega-conotoxins MVIIA, MVIIC and 14 loop splice hybrids at N and P/Q-type calcium channels., Nielsen KJ, Adams D, Thomas L, Bond T, Alewood PF, Craik DJ, Lewis RJ, J Mol Biol. 1999 Jun 25;289(5):1405-21. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/10373375 10373375] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Adams, D.]] | [[Category: Adams, D.]] | ||
| Line 20: | Line 29: | ||
[[Category: Thomas, L.]] | [[Category: Thomas, L.]] | ||
[[Category: NH2]] | [[Category: NH2]] | ||
[[Category: peptide | [[Category: peptide hybrid]] | ||
[[Category: voltage-sensitive calcium channel antagonist]] | [[Category: voltage-sensitive calcium channel antagonist]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 10:26:39 2008'' | ||
Revision as of 08:26, 20 March 2008
| |||||||||||||
| 1cnn | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Ligands: | NH2 | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
OMEGA-CONOTOXIN MVIIC FROM CONUS MAGUS
Overview
The omega-conotoxins are a set of structurally related, four-loop, six cysteine containing peptides, that have a range of selectivities for different subtypes of the voltage-sensitive calcium channel (VSCC). To investigate the basis of the selectivity displayed by these peptides, we have studied the binding affinities of two naturally occurring omega-conotoxins, MVIIA and MVIIC and a series of 14 MVIIA/MVIIC loop hybrids using radioligand binding assays for N and P/Q-type Ca2+channels in rat brain tissue. A selectivity profile was developed from the ratio of relative potencies at N-type VSCCs (using [125I]GVIA radioligand binding assays) and P/Q-type VSCCs (using [125I]MVIIC radioligand binding assays). In these peptides, loops 2 and 4 make the greatest contribution to VSCC subtype selectivity, while the effects of loops 1 and 3 are negligible. Peptides with homogenous combinations of loop 2 and 4 display clear selectivity preferences, while those with heterogeneous combinations of loops 2 and 4 are less discriminatory. 1H NMR spectroscopy revealed that the global folds of MVIIA, MVIIC and the 14 loop hybrid peptides were similar; however, several differences in local structure were identified. Based on the binding data and the 3D structures of MVIIA, GVIA and MVIIC, we have developed a preliminary pharmacophore based on the omega-conotoxin residues most likely to interact with the N-type VSCC.
About this Structure
1CNN is a Single protein structure of sequence from [1]. Full crystallographic information is available from OCA.
Reference
Structure-activity relationships of omega-conotoxins MVIIA, MVIIC and 14 loop splice hybrids at N and P/Q-type calcium channels., Nielsen KJ, Adams D, Thomas L, Bond T, Alewood PF, Craik DJ, Lewis RJ, J Mol Biol. 1999 Jun 25;289(5):1405-21. PMID:10373375
Page seeded by OCA on Thu Mar 20 10:26:39 2008
