Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
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 displa...
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| Veröffentlicht in: | Journal of medicinal chemistry 2016-06, Vol.59 (11), p.5149-5157 |
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| container_title | Journal of medicinal chemistry |
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| creator | Vivier, Delphine Bennis, Khalil Lesage, Florian Ducki, Sylvie |
| description | 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. |
| doi_str_mv | 10.1021/acs.jmedchem.5b00671 |
| format | Article |
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We review the TREK-1 channel, its structural and functional properties, and the pharmacological agents (agonists and antagonists) able to modulate its gating.</description><subject>Arrhythmias, Cardiac - drug therapy</subject><subject>Depression - drug therapy</subject><subject>Epilepsy - drug therapy</subject><subject>Humans</subject><subject>Inflammation - drug therapy</subject><subject>Models, Molecular</subject><subject>Molecular Structure</subject><subject>Neuroprotective Agents - chemistry</subject><subject>Neuroprotective Agents - pharmacology</subject><subject>Pain - drug therapy</subject><subject>Potassium Channels, Tandem Pore Domain - agonists</subject><subject>Potassium Channels, Tandem Pore Domain - antagonists & inhibitors</subject><subject>Potassium Channels, Tandem Pore Domain - metabolism</subject><subject>Structure-Activity Relationship</subject><issn>1520-4804</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo90F1LwzAYBeAgiJvTfyCSyw1pzds2SXslY04dGzpGwcuSpG9dR79s2g3_vROnVwcOD-fiEHIDzAXmwb0y1t2VmJotli7XjAkJZ2QI3GNOELJgQC6t3THGfPD8CzLwBA-PNR-Swxpb26Dp8j1aWle02yKND7Wzrlukj3Wp8oqu605Zm_clnW1VVWFB48186QAdx--LpbPBQnWY0uX4bvIvYOLSKX2t9z96i61qsO9yQ2PVfmD3cEXOM1VYvD7liMRP83j24qzenhez6cppuOCOAClNplCiTGXAM6GDLAo0F1obPwIIBZg0VQyENDpgkeYMDKReBJJBJlJ_RMa_s01bf_Zou6TMrcGiUBXWvU1ARjwUkRfyI7090V4fr0yaNi9V-5X8feV_A0psado</recordid><startdate>20160609</startdate><enddate>20160609</enddate><creator>Vivier, Delphine</creator><creator>Bennis, Khalil</creator><creator>Lesage, Florian</creator><creator>Ducki, Sylvie</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>20160609</creationdate><title>Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). 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| subjects | Arrhythmias, Cardiac - drug therapy Depression - drug therapy Epilepsy - drug therapy Humans Inflammation - drug therapy Models, Molecular Molecular Structure Neuroprotective Agents - chemistry Neuroprotective Agents - pharmacology Pain - drug therapy Potassium Channels, Tandem Pore Domain - agonists Potassium Channels, Tandem Pore Domain - antagonists & inhibitors Potassium Channels, Tandem Pore Domain - metabolism Structure-Activity Relationship |
| title | Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target? |
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