Chemical tools for K(+) channel biology

Christopher A Ahern; William R Kobertz

doi:10.1021/bi8018515

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Journal article

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Peer reviewed

Chemical tools for K(+) channel biology

Christopher A Ahern and William R Kobertz

Biochemistry (Easton), Vol.48(3), pp.517-526

01/27/2009

DOI: 10.1021/bi8018515

PMCID: PMC2629505

PMID: 19113860

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Abstract

K(+) channels are revered for their universal action of suppressing electrical activity in nerve and muscle, as well as regulating salt and water transport in epithelial tissues involved in metabolism and digestion. These multisubunit membrane-embedded proteins carry out their physiological chore, selectively allowing the passage of potassium across the membrane, in response to changes in membrane voltage and ligand concentration. Elucidating the diverse gating properties of K(+) channels is of great biological interest since their molecular motions provide insight into how these structurally similar proteins function in a wide variety of tissues. Armed with patch clamps, chart recorders, and now high-resolution structures, electrophysiologists have been dipping into the top tray of the chemist's tool box: synthesizing cysteine-modifying agents and organic cations and grinding up insects, spiders, and other vermin to isolate natural products to poke, probe, and prod K(+) channels. Recently, there has been further cross-fertilization between chemists and K(+) channelologists, resulting in greater accessibility to more elaborate synthetic methodologies and screening approaches. In this review, we catalogue the evolution of chemical tools and approaches that have been utilized to elucidate the mechanistic underpinnings of K(+) channel biology.

Potassium Channels - metabolism

Amino Acids - metabolism

Small Molecule Libraries

Humans

Potassium Channel Blockers - pharmacology

Protein Subunits - metabolism

Quaternary Ammonium Compounds - pharmacology

Details

Title: Subtitle: Chemical tools for K(+) channel biology
Creators: Christopher A Ahern - Department of Anesthesiology, University of British Columbia, 2350 Health Science Mall, Vancouver, BC V6T 1Z3, Canada. cahern@interchange.ubc.ca
William R Kobertz
Resource Type: Journal article
Publication Details: Biochemistry (Easton), Vol.48(3), pp.517-526
DOI: 10.1021/bi8018515
PMID: 19113860
PMCID: PMC2629505
NLM abbreviation: Biochemistry
ISSN: 0006-2960
eISSN: 1520-4995
Publisher: United States
Grant note: R01 DC007669-04 / NIDCD NIH HHS DC-007669 / NIDCD NIH HHS R01 DC007669 / NIDCD NIH HHS R01 GM070650-04 / NIGMS NIH HHS GM-070650 / NIGMS NIH HHS R01 GM070650 / NIGMS NIH HHS
Language: English
Date published: 01/27/2009
Academic Unit: Molecular Physiology and Biophysics; Iowa Neuroscience Institute
Record Identifier: 9984070745102771

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