KcsA钾通道的快速细胞内四乙铵阻断
Rapid intracellular TEA block of the KcsA potassium channel.
作者信息
Kutluay Esin, Roux Benoît, Heginbotham Lise
机构信息
Department of Biochemistry, Weill Graduate School of Medical Sciences, Cornell University, New York, New York 10021, USA.
出版信息
Biophys J. 2005 Feb;88(2):1018-29. doi: 10.1529/biophysj.104.052043. Epub 2004 Nov 19.
Abstract
Intracellular tetraethylammonium (TEA) inhibition was studied at the single-channel level in the KcsA potassium channel reconstituted in planar lipid bilayers. TEA acts as a fast blocker (resulting in decreased current amplitude) with an affinity in the 75 mM range even at high bandwidth. Studies over a wide voltage range reveal that TEA block has a complex voltage-dependence that also depends on the ionic conditions. These observations are examined in the context of permeation models to extend our understanding of the coupling between permeant ions and TEA blockade.
摘要
在平面脂质双分子层中重组的KcsA钾通道的单通道水平上研究了细胞内四乙铵（TEA）抑制作用。即使在高带宽下，TEA也作为一种快速阻滞剂（导致电流幅度降低），其亲和力在75 mM范围内。在很宽的电压范围内进行的研究表明，TEA阻断具有复杂的电压依赖性，这也取决于离子条件。在渗透模型的背景下对这些观察结果进行了研究，以扩展我们对渗透离子与TEA阻断之间耦合的理解。
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本文引用的文献
1
All-atom empirical potential for molecular modeling and dynamics studies of proteins.
J Phys Chem B. 1998 Apr 30;102(18):3586-616. doi: 10.1021/jp973084f.
2
Unique inner pore properties of BK channels revealed by quaternary ammonium block.
J Gen Physiol. 2004 Jul;124(1):43-57. doi: 10.1085/jgp.200409067. Epub 2004 Jun 14.
3
Ion binding affinity in the cavity of the KcsA potassium channel.
Biochemistry. 2004 May 4;43(17):4978-82. doi: 10.1021/bi049876z.
4
Intracellular gate opening in Shaker K+ channels defined by high-affinity metal bridges.
Nature. 2004 Apr 22;428(6985):864-8. doi: 10.1038/nature02468.
5
ANOMALOUS RECTIFICATION IN THE SQUID GIANT AXON INJECTED WITH TETRAETHYLAMMONIUM CHLORIDE.
J Gen Physiol. 1965 May;48(5):859-72. doi: 10.1085/jgp.48.5.859.
6
External TEA block of shaker K+ channels is coupled to the movement of K+ ions within the selectivity filter.
J Gen Physiol. 2003 Aug;122(2):239-46. doi: 10.1085/jgp.200308848.
7
A microscopic view of ion conduction through the K+ channel.
Proc Natl Acad Sci U S A. 2003 Jul 22;100(15):8644-8. doi: 10.1073/pnas.1431750100. Epub 2003 Jul 1.
8
Functional identification of ion binding sites at the internal end of the pore in Shaker K+ channels.
J Physiol. 2003 May 15;549(Pt 1):107-20. doi: 10.1113/jphysiol.2002.038646. Epub 2003 Mar 28.
9
Opening the KcsA K+ channel: tryptophan scanning and complementation analysis lead to mutants with altered gating.
Biochemistry. 2002 Nov 19;41(46):13653-62. doi: 10.1021/bi026393r.
10
Na+ block and permeation in a K+ channel of known structure.
J Gen Physiol. 2002 Sep;120(3):323-35. doi: 10.1085/jgp.20028614.
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