ArticleThe Journal of physiology2002
Multiple inhibitory effects of Au(CN)(2-) ions on cystic fibrosis transmembrane conductance regulator Cl(-) channel currents.
Article in The Journal of physiology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Location of a permeant anion binding site in the cystic fibrosis transmembrane conductance regulator chloride channel pore.The journal of physiological sciences : JPS · 2015Article
- State-dependent blocker interactions with the CFTR chloride channel: implications for gating the pore.Pflugers Archiv : European journal of physiology · 2014Article
- Functional differences in pore properties between wild-type and cysteine-less forms of the CFTR chloride channel.The Journal of membrane biology · 2011Article
- Functional arrangement of the 12th transmembrane region in the CFTR chloride channel pore based on functional investigation of a cysteine-less CFTR variant.Pflugers Archiv : European journal of physiology · 2011Article
- Alignment of transmembrane regions in the cystic fibrosis transmembrane conductance regulator chloride channel pore.The Journal of general physiology · 2011Article
- Polystyrene nanoparticles activate ion transport in human airway epithelial cells.International journal of nanomedicine · 2011Article
- Changes in accessibility of cytoplasmic substances to the pore associated with activation of the cystic fibrosis transmembrane conductance regulator chloride channel.The Journal of biological chemistry · 2010Article
- Regulation of conductance by the number of fixed positive charges in the intracellular vestibule of the CFTR chloride channel pore.The Journal of general physiology · 2010Article
- Cysteine-independent inhibition of the CFTR chloride channel by the cysteine-reactive reagent sodium (2-sulphonatoethyl) methanethiosulphonate.British journal of pharmacology · 2009Article
- Novel residues lining the CFTR chloride channel pore identified by functional modification of introduced cysteines.The Journal of membrane biology · 2009Article
- Identification of positive charges situated at the outer mouth of the CFTR chloride channel pore.Pflugers Archiv : European journal of physiology · 2008Article
- On the origin of asymmetric interactions between permeant anions and the cystic fibrosis transmembrane conductance regulator chloride channel pore.Biophysical journal · 2007Article
- CFTR: Ligand exchange between a permeant anion ([Au(CN)2]-) and an engineered cysteine (T338C) blocks the pore.Biophysical journal · 2006Article
- Interactions between impermeant blocking ions in the cystic fibrosis transmembrane conductance regulator chloride channel pore: evidence for anion-induced conformational changes.The Journal of membrane biology · 2006Article
- Mutation-induced blocker permeability and multiion block of the CFTR chloride channel pore.The Journal of general physiology · 2003Article
- Voltage-dependent gating of the cystic fibrosis transmembrane conductance regulator Cl- channel.The Journal of general physiology · 2003Article
- Coupled movement of permeant and blocking ions in the CFTR chloride channel pore.The Journal of physiology · 2003Article
- Molecular determinants and role of an anion binding site in the external mouth of the CFTR chloride channel pore.The Journal of physiology · 2003Article
- Probing an open CFTR pore with organic anion blockers.The Journal of general physiology · 2002Article
- Mechanism of lonidamine inhibition of the CFTR chloride channel.British journal of pharmacology · 2002Article
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Authors and funding
2 authors.
Funding
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Abstract
Lyotropic pseudohalide anions are potentially useful as high affinity probes of Cl(-) channel pores. However, the interaction between these pseudohalides and the cystic fibrosis transmembrane conductance regulator (CFTR) Cl(-) channel have not been described in detail. Here we show that Au(CN)(2-) ions applied to the intracellular face of membrane patches from stably transfected baby hamster kidney cells inhibit CFTR channel currents by at least two mechanisms, which can be distinguished at the single channel level or by inhibiting channel closure using 2 mM pyrophosphate. Low concentrations (< 10 microM) of Au(CN)(2-) significantly reduced CFTR channel open probability. This effect was apparently voltage insensitive, independent of extracellular Cl(-) concentration, and lost following exposure to pyrophosphate. Higher concentrations of intracellular Au(CN)(2-) caused an apparent reduction in unitary current amplitude, presumably due to a kinetically fast blocking reaction. This effect, isolated following exposure to pyrophosphate, was strongly voltage dependent (apparent K(d) 61.6 microM at -100 mV and 913 microM at +60 mV). Both the affinity and voltage dependence of block were highly sensitive to extracellular Cl(-) concentration. We propose that Au(CN)(2-) has at least two inhibitory effects on CFTR currents: a high affinity effect on channel gating due to action on a cytoplasmically accessible aspect of the channel and a lower affinity block within the open channel pore. These results offer important caveats for the use of lyotropic pseudohalide anions such as Au(CN)(2-) as specific high affinity probes of Cl(-) channel pores.
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