Reconstitution of the voltage-gated K+ channel KAT1 in planar lipid bilayers

2008 ◽  
Vol 10 (10) ◽  
pp. 1509-1512 ◽  
Author(s):  
Shunsuke Ozaki ◽  
Shiho Aoki ◽  
Takao Hibi ◽  
Kenji Kano ◽  
Osamu Shirai
Keyword(s):  
Lipid Bilayers ◽  
K Channel ◽  
Planar Lipid Bilayers ◽  
Voltage Gated

Effect of phospholipid surface charge on the conductance and gating of a Ca2+-activated K+ channel in planar lipid bilayers

1985 ◽  
Vol 83 (3) ◽  
pp. 273-282 ◽  
Author(s):  
Edward Moczydlowski ◽  
Osvaldo Alvarez ◽  
Cecilia Vergara ◽  
Ramon Latorre
Keyword(s):  
Surface Charge ◽  
Lipid Bilayers ◽  
K Channel ◽  
Planar Lipid Bilayers

scholarly journals Synthetic Analogs of the Snail Toxin 6-Bromo-2-Mercaptotryptamine Dimer (BrMT) Reveal That Lipid Bilayer Perturbation Does Not Underlie Its Modulation of Voltage-Gated Potassium Channels

2018 ◽  
Author(s):  
Chris Dockendorff ◽  
Disha M. Gandhi ◽  
Ian H. Kimball ◽  
Kenneth S. Eum ◽  
Radda Rusinova ◽  
...  
Keyword(s):  
Lipid Bilayer ◽  
Lipid Bilayers ◽  
Medicinal Chemistry ◽  
K Channel ◽  
Channel Activity ◽  
Synthetic Analogs ◽  
Voltage Gated ◽  
Protein Ligand Interactions ◽  
Membrane Perturbation ◽  
Ligand Interactions

Distinguishing membrane perturbation from more direct protein-ligand interactions is an ongoing challenge in chemical biology. Herein, we present one strategy for doing so, using dimeric 6-bromo-2-mercaptotryptamine (BrMT) and synthetic analogs. BrMT is a chemically unstable marine snail toxin that has unique effects on voltage-gated K+ channel proteins, making it an attractive medicinal chemistry lead. BrMT is amphiphilic and perturbs lipid bilayers, raising the question of whether its action against K+ channels is merely a manifestation of membrane perturbation. To determine whether medicinal chemistry approaches to improve BrMT might be viable, we synthesized BrMT and 11 analogs and determined their activities in parallel assays measuring K+ channel activity and lipid bilayer properties. Our work demonstrates a strategy for determining if drugs act by specific interactions or bilayer-dependent mechanisms, and chemically stable modulators of Kv1 channels are reported.

scholarly journals Synthetic Analogs of the Snail Toxin 6-Bromo-2-Mercaptotryptamine Dimer (BrMT) Reveal That Lipid Bilayer Perturbation Does Not Underlie Its Modulation of Voltage-Gated Potassium Channels

2018 ◽  
Author(s):  
Chris Dockendorff ◽  
Disha M. Gandhi ◽  
Ian H. Kimball ◽  
Kenneth S. Eum ◽  
Radda Rusinova ◽  
...  
Keyword(s):  
Lipid Bilayer ◽  
Lipid Bilayers ◽  
Medicinal Chemistry ◽  
K Channel ◽  
Channel Activity ◽  
Synthetic Analogs ◽  
Voltage Gated ◽  
Protein Ligand Interactions ◽  
Membrane Perturbation ◽  
Ligand Interactions

Distinguishing membrane perturbation from more direct protein-ligand interactions is an ongoing challenge in chemical biology. Herein, we present one strategy for doing so, using dimeric 6-bromo-2-mercaptotryptamine (BrMT) and synthetic analogs. BrMT is a chemically unstable marine snail toxin that has unique effects on voltage-gated K+ channel proteins, making it an attractive medicinal chemistry lead. BrMT is amphiphilic and perturbs lipid bilayers, raising the question of whether its action against K+ channels is merely a manifestation of membrane perturbation. To determine whether medicinal chemistry approaches to improve BrMT might be viable, we synthesized BrMT and 11 analogs and determined their activities in parallel assays measuring K+ channel activity and lipid bilayer properties. Our work demonstrates a strategy for determining if drugs act by specific interactions or bilayer-dependent mechanisms, and chemically stable modulators of Kv1 channels are reported.

Pf3 coat protein forms voltage-gated ion channels in planar lipid bilayers

Biochemistry ◽  
1994 ◽  
Vol 33 (1) ◽  
pp. 283-290 ◽  
Author(s):  
Michael Pawlak ◽  
Andreas Kuhn ◽  
Horst Vogel
Keyword(s):  
Ion Channels ◽  
Coat Protein ◽  
Lipid Bilayers ◽  
Planar Lipid Bilayers ◽  
Voltage Gated ◽  
Voltage Gated Ion Channels ◽  
Gated Ion Channels

Single K+-channel current measurements from brain synaptosomes in lipid bilayers

1983 ◽  
Vol 245 (1) ◽  
pp. C151-C156 ◽  
Author(s):  
M. T. Nelson ◽  
M. Roudna ◽  
E. Bamberg
Keyword(s):  
Ion Channels ◽  
Lipid Bilayers ◽  
Single Channel ◽  
Mammalian Brain ◽  
K Channel ◽  
Kinetic Properties ◽  
Nerve Terminals ◽  
Planar Lipid Bilayers ◽  
Presynaptic Nerve Terminals ◽  
Single Channel Currents

Ion channels from a rat brain preparation enriched in presynaptic nerve terminals (synaptosomes) were incorporated into planar lipid bilayers. Experiments examined macroscopic (channel-ensemble) currents as well as single-channel currents. Four single-channel conductances (ranging from 10 to 40 pS) were usually observed, each with distinct kinetic properties. All the observed channels selected for K+ over Cl-. These K+ channels may contribute to the resting K+ conductance of brain nerve terminals. Furthermore, this report demonstrates that the properties of ion channels from mammalian brain can be studied in planar lipid bilayers and suggests that this system can be readily extended to many additional investigations on the electrical properties of brain membranes.

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