1cnn

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{{STRUCTURE_1cnn| PDB=1cnn | SCENE= }}
{{STRUCTURE_1cnn| PDB=1cnn | SCENE= }}
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'''OMEGA-CONOTOXIN MVIIC FROM CONUS MAGUS'''
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===OMEGA-CONOTOXIN MVIIC FROM CONUS MAGUS===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 10373375 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10373375}}
==About this Structure==
==About this Structure==
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1CNN is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1CNN OCA].
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1CNN is a [[Single protein]] structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1CNN OCA].
==Reference==
==Reference==
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[[Category: Peptide hybrid]]
[[Category: Peptide hybrid]]
[[Category: Voltage-sensitive calcium channel antagonist]]
[[Category: Voltage-sensitive calcium channel antagonist]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 20:59:21 2008''

Revision as of 17:59, 30 June 2008

Template:STRUCTURE 1cnn

OMEGA-CONOTOXIN MVIIC FROM CONUS MAGUS

Template:ABSTRACT PUBMED 10373375

About this Structure

1CNN is a Single protein structure. Full experimental 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

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