Photochromic Blockers of Voltage-Gated Potassium Channels

Light work: Studies into the mechanism of AAQ, a photoswitchable blocker of voltage‐gated K+ channels, led to the discovery and development of photochromic ligands that act at the internal tetraethylammonium binding site (see picture). These molecules can be applied from the extracellular side to im...

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Published inAngewandte Chemie (International ed.) Vol. 48; no. 48; pp. 9097 - 9101
Main Authors Banghart, Matthew R, Mourot, Alexandre, Fortin, Doris L, Yao, Jennifer Z, Kramer, Richard H, Trauner, Dirk
Format Journal Article
LanguageEnglish
Published Weinheim Wiley-VCH Verlag 01.01.2009
WILEY-VCH Verlag
WILEY‐VCH Verlag
Wiley
Subjects
azo compounds
Binding Sites
Cell Line
Chemistry
Chemistry, Multidisciplinary
Hippocampus - drug effects
Hippocampus - metabolism
Humans
ion channels
Isomerism
Ligands
Molecular Structure
open-channel block
Patch-Clamp Techniques
photochromism
Photosensitizing Agents - chemistry
Photosensitizing Agents - pharmacology
Physical Sciences
Potassium Channel Blockers - chemistry
Potassium Channel Blockers - pharmacology
Potassium Channels, Voltage-Gated - antagonists & inhibitors
Potassium Channels, Voltage-Gated - metabolism
Science & Technology
Structure-Activity Relationship
structure-activity relationships
CONDUCTANCE
SITE
ANTAGONIST
photochromism
azo compounds
ANOMALOUS RECTIFICATION
ion channels
ACETYLCHOLINE-RECEPTOR
TEA BLOCKADE
open-channel block
INACTIVATION
structure-activity relationships
K+-CHANNELS
GIANT AXONS
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Summary:Light work: Studies into the mechanism of AAQ, a photoswitchable blocker of voltage‐gated K+ channels, led to the discovery and development of photochromic ligands that act at the internal tetraethylammonium binding site (see picture). These molecules can be applied from the extracellular side to impart long‐lasting photosensitivity on K+ channels in living cells and thereby afford photocontrol of action potential firing in neurons.
Bibliography:http://dx.doi.org/10.1002/anie.200904504
ark:/67375/WNG-2F9BMR50-7
This work was supported by a Laboratory Directed Research Development Award from the Lawrence Berkeley National Laboratory (R.H.K.), NSF-DFG grant CHE0724214 (D.T.), the National Institutes of Health Nanomedicine Development Center for the Optical Control of Biological Function (5PN2EY018241; R.H.K. and D.T.), and by a grant from the Human Frontier Science Program (RGP23-2005; R.H.K. and D.T.). We thank F. Tombola and E. Isacoff for insightful discussions, the Isacoff and Yellen laboratories for Shaker clones, and T. Fehrentz for additional experiments (not included).
Lawrence Berkeley National Laboratory
National Institutes of Health - No. 5PN2EY018241
NSF-DFG - No. CHE0724214
istex:3A28FC4AEFB2B3EE9254A97FF9E56BB1D9445FCF
Human Frontier Science Program - No. RGP23-2005
ArticleID:ANIE200904504
These authors contributed equally to this work.
This work was supported by a Laboratory Directed Research Development Award from the Lawrence Berkeley National Laboratory (R.H.K.), NSF‐DFG grant CHE0724214 (D.T.), the National Institutes of Health Nanomedicine Development Center for the Optical Control of Biological Function (5PN2EY018241; R.H.K. and D.T.), and by a grant from the Human Frontier Science Program (RGP23‐2005; R.H.K. and D.T.). We thank F. Tombola and E. Isacoff for insightful discussions, the Isacoff and Yellen laboratories for Shaker clones, and T. Fehrentz for additional experiments (not included).
NIH RePORTER
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200904504