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| [[Image:1cnn.gif|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_1cnn| PDB=1cnn | SCENE= }} | | {{STRUCTURE_1cnn| PDB=1cnn | SCENE= }} |
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| '''OMEGA-CONOTOXIN MVIIC FROM CONUS MAGUS'''
| | ===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. | | The line below this paragraph, {{ABSTRACT_PUBMED_10373375}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 10373375 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_10373375}} |
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| ==About this Structure== | | ==About this Structure== |
| 1CNN is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1CNN OCA]. | | 1CNN is a [[Single protein]] structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1CNN OCA]. |
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| ==Reference== | | ==Reference== |
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| [[Category: Peptide hybrid]] | | [[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 Fri May 2 12:55:27 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 20:59:21 2008'' |
