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Molecular and functional properties of two-pore-domain potassium channels

Molecular and functional properties of two-pore-domain potassium channels Abstract The two-pore-domain K + channels, or K 2P channels, constitute a novel class of K + channel subunits. They have four transmembrane segments and are active as dimers. The tissue distribution of these channels is widespread, and they are found in both excitable and nonexcitable cells. K 2P channels produce currents with unusual characteristics. They are quasi-instantaneous and noninactivating, and they are active at all membrane potentials and insensitive to the classic K + channel blockers. These properties designate them as background K + channels. They are expected to play a major role in setting the resting membrane potential in many cell types. Another salient feature of K 2P channels is the diversity of their regulatory mechanisms. The weak inward rectifiers TWIK-1 and TWIK-2 are stimulated by activators of protein kinase C and decreased by internal acidification, the baseline TWIK-related acid-sensitive K + (TASK)-1 and TASK-2 channels are sensitive to external pH changes in a narrow range near physiological pH, and the TWIK-related (TREK)-1 and TWIK-related arachidonic acid-stimulated K + (TRAAK) channels are the first cloned polyunsaturated fatty acids-activated and mechanogated K + channels. The recent demonstration that TASK-1 and TREK-1 channels are activated by inhalational general anesthetics, and that TRAAK is activated by the neuroprotective agent riluzole, indicates that this novel class of K + channels is an interesting target for new therapeutic developments. two-pore-domain channels mechanosensitivity anesthetics Footnotes Address for reprint requests and other correspondence: M. Lazdunski, Institut de Pharmacologie Moléculaire et Cellulaire, Centre National de la Recherche Scientifique-660, Route des Lucioles, 06560 Valbonne, France (E-mail: [email protected] ). The costs of publication of this article were defrayed in part by the payment of page charges. The article must therefore be hereby marked “ advertisement ” in accordance with 18 U.S.C. Section 1734 solely to indicate this fact. Copyright © 2000 the American Physiological Society http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png AJP - Renal Physiology The American Physiological Society

Molecular and functional properties of two-pore-domain potassium channels

Lesage, Florian; Lazdunski, Michel
AJP - Renal Physiology , Volume 279 (5): F793 – Nov 1, 2000
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Publisher
The American Physiological Society
Copyright
Copyright © 2011 the American Physiological Society
ISSN
0363-6127
eISSN
1522-1466
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Abstract

Abstract The two-pore-domain K + channels, or K 2P channels, constitute a novel class of K + channel subunits. They have four transmembrane segments and are active as dimers. The tissue distribution of these channels is widespread, and they are found in both excitable and nonexcitable cells. K 2P channels produce currents with unusual characteristics. They are quasi-instantaneous and noninactivating, and they are active at all membrane potentials and insensitive to the classic K + channel blockers. These properties designate them as background K + channels. They are expected to play a major role in setting the resting membrane potential in many cell types. Another salient feature of K 2P channels is the diversity of their regulatory mechanisms. The weak inward rectifiers TWIK-1 and TWIK-2 are stimulated by activators of protein kinase C and decreased by internal acidification, the baseline TWIK-related acid-sensitive K + (TASK)-1 and TASK-2 channels are sensitive to external pH changes in a narrow range near physiological pH, and the TWIK-related (TREK)-1 and TWIK-related arachidonic acid-stimulated K + (TRAAK) channels are the first cloned polyunsaturated fatty acids-activated and mechanogated K + channels. The recent demonstration that TASK-1 and TREK-1 channels are activated by inhalational general anesthetics, and that TRAAK is activated by the neuroprotective agent riluzole, indicates that this novel class of K + channels is an interesting target for new therapeutic developments. two-pore-domain channels mechanosensitivity anesthetics Footnotes Address for reprint requests and other correspondence: M. Lazdunski, Institut de Pharmacologie Moléculaire et Cellulaire, Centre National de la Recherche Scientifique-660, Route des Lucioles, 06560 Valbonne, France (E-mail: [email protected] ). The costs of publication of this article were defrayed in part by the payment of page charges. The article must therefore be hereby marked “ advertisement ” in accordance with 18 U.S.C. Section 1734 solely to indicate this fact. Copyright © 2000 the American Physiological Society

Journal

AJP - Renal Physiology – The American Physiological Society

Published: Nov 1, 2000

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