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Norfluoxetine inhibits TREK-2 K2P channels by multiple mechanisms including state-independent effects on the selectivity filter gate

Abstract:

The TREK subfamily of two-pore domain K+ (K2P) channels are inhibited by fluoxetine and its metabolite, norfluoxetine (NFx). Although not the principal targets of this antidepressant, TREK channel inhibition by NFx has provided important insights into the conformational changes associated with channel gating and highlighted the role of the selectivity filter in this process. However, despite the availability of TREK-2 crystal structures with NFx bound, the precise mechanisms underlying NFx in...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1085/jgp.202012812

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Institution:
University of Oxford
Department:
PHYSICS
Sub department:
AV PHYSIOLOGY ANATOMY AND GENETICS; DK CONDENSED MATTER PHYSICS
Role:
Author
ORCID:
0000-0001-6097-3646
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Role:
Author
ORCID:
0000-0002-6192-5651
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Role:
Author
ORCID:
0000-0001-5175-1988
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Role:
Author
ORCID:
0000-0003-4892-5523
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Publisher:
Rockefeller University Press Publisher's website
Journal:
Journal of General Physiology Journal website
Volume:
153
Issue:
8
Article number:
e202012812
Place of publication:
United States
Publication date:
2021-05-25
Acceptance date:
2021-05-06
DOI:
EISSN:
1540-7748
ISSN:
0022-1295
Pmid:
34032848
Language:
English
Keywords:
Pubs id:
1179170
Local pid:
pubs:1179170
Deposit date:
2021-07-22

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