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2A9H

NMR structural studies of a potassium channel / charybdotoxin complex

2A9H の概要
エントリーDOI10.2210/pdb2a9h/pdb
NMR情報BMRB: 6728
分子名称Voltage-gated potassium channel, charybdotoxin (2 entities in total)
機能のキーワードpotassium channel, kcsa, membrane protein, metal transport
由来する生物種Streptomyces lividans
タンパク質・核酸の鎖数5
化学式量合計71179.89
構造登録者
Yu, L.,Sun, C.,Song, D.,Shen, J.,Xu, N.,Gunasekera, A.,Hajduk, P.J.,Olejniczak, E.T. (登録日: 2005-07-11, 公開日: 2006-01-10, 最終更新日: 2024-11-20)
主引用文献Yu, L.,Sun, C.,Song, D.,Shen, J.,Xu, N.,Gunasekera, A.,Hajduk, P.J.,Olejniczak, E.T.
Nuclear magnetic resonance structural studies of a potassium channel-charybdotoxin complex.
Biochemistry, 44:15834-15841, 2005
Cited by
PubMed Abstract: 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.
PubMed: 16313186
DOI: 10.1021/bi051656d
主引用文献が同じPDBエントリー
実験手法
SOLUTION NMR
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件を2025-07-02に公開中

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