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Journal article

K2P channel gating mechanisms revealed by structures of TREK-2 and a complex with Prozac

Abstract:

TREK-2 (KCNK10/K2P10), a two-pore domain potassium (K2P) channel, is gated by multiple stimuli such as stretch, fatty acids, and pH and by several drugs. However, the mechanisms that control channel gating are unclear. Here we present crystal structures of the human TREK-2 channel (up to 3.4 angstrom resolution) in two conformations and in complex with norfluoxetine, the active metabolite of fluoxetine (Prozac) and a state-dependent blocker of TREK channels. Norfluoxetine binds within intrame...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1126/science.1261512

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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
ORCID:
0000-0001-9661-2607
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Role:
Author
ORCID:
0000-0002-0859-3854
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Wellcome Trust More from this funder
Boehringer Ingelheim More from this funder
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Publisher:
American Association for the Advancement of Science Publisher's website
Journal:
Science Journal website
Volume:
347
Issue:
6227
Pages:
1256-1259
Publication date:
2015-03-13
Acceptance date:
2015-02-05
DOI:
EISSN:
1095-9203
ISSN:
0036-8075
Pmid:
25766236
Source identifiers:
512806
Language:
English
Keywords:
Pubs id:
pubs:512806
UUID:
uuid:274e687e-390c-44a8-9f9b-7fa235ed669c
Local pid:
pubs:512806
Deposit date:
2018-10-25

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