Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K+ Channel 1). A Novel Therapeutic Target?

Abstract : Potassium (K+) channels are membrane proteins expressed in most living cells that selectively control the flow of K+ ions. More than 80 genes encode the K+ channel subunits in the human genome. The TWIK-related K+ channel (TREK-1) belongs to the two-pore domain K+ channels (K2P) and displays various properties including sensitivity to physical (membrane stretch, acidosis, temperature) and chemical stimuli (signaling lipids, volatile anesthetics). The distribution of TREK-1 in the central nervous system, coupled with the physiological consequences of its opening and closing, leads to the emergence of this channel as an attractive therapeutic target. We review the TREK-1 channel, its structural and functional properties, and the pharmacological agents (agonists and antagonists) able to modulate its gating.
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Submitted on : Tuesday, July 26, 2016 - 4:34:13 PM
Last modification on : Thursday, May 3, 2018 - 1:34:01 PM

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Delphine Vivier, Khalil Bennis, Florian Lesage, Sylvie Ducki. Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K+ Channel 1). A Novel Therapeutic Target? . Journal of Medicinal Chemistry, American Chemical Society, 2016, 59, pp.5149-5157. ⟨10.1021/acs.jmedchem.5b00671⟩. ⟨hal-01349091⟩

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