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2a9h

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{{STRUCTURE_2a9h| PDB=2a9h | SCENE= }}
{{STRUCTURE_2a9h| PDB=2a9h | SCENE= }}
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'''NMR structural studies of a potassium channel / charybdotoxin complex'''
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===NMR structural studies of a potassium channel / charybdotoxin complex===
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==Overview==
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Ion channels play critical roles in signaling processes and are attractive targets for treating various diseases. Here we describe an NMR-based strategy for structural analyses of potassium channel-ligand complexes using KcsA (residues 1-132, with six mutations to impart toxin binding and to mimic the eukaryotic hERG channel). Using this approach, we determined the solution structure of KcsA in complex with the high-affinity peptide antagonist charybdotoxin. The structural data reveal how charybdotoxin binds to the closed form of KcsA and makes specific contacts with the extracellular surface of the ion channel, resulting in pore blockage. This represents the first direct structural information about an ion channel complexed to a peptide antagonist and provides an experimental framework for understanding and interpreting earlier mutational analyses. The strategy presented here overcomes many of the limitations of conventional NMR approaches to helical membrane protein structure determination and can be applied in the study of the binding of druglike molecules to this important class of proteins.
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{{ABSTRACT_PUBMED_16313186}}
==About this Structure==
==About this Structure==
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2A9H is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Streptomyces_lividans Streptomyces lividans]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2A9H OCA].
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2A9H is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Streptomyces_lividans Streptomyces lividans]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2A9H OCA].
==Reference==
==Reference==
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[[Category: Potassium channel]]
[[Category: Potassium channel]]
[[Category: Structure]]
[[Category: Structure]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 19:00:45 2008''

Revision as of 16:00, 28 July 2008

Image:2a9h.png

Template:STRUCTURE 2a9h

NMR structural studies of a potassium channel / charybdotoxin complex

Template:ABSTRACT PUBMED 16313186

About this Structure

2A9H is a Single protein structure of sequence from Streptomyces lividans. Full experimental information is available from OCA.

Reference

Nuclear magnetic resonance structural studies of a potassium channel-charybdotoxin complex., Yu L, Sun C, Song D, Shen J, Xu N, Gunasekera A, Hajduk PJ, Olejniczak ET, Biochemistry. 2005 Dec 6;44(48):15834-41. PMID:16313186

Page seeded by OCA on Mon Jul 28 19:00:45 2008

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