Loading
PDBj
MenuPDBj@FacebookPDBj@X(formerly Twitter)PDBj@BlueSkyPDBj@YouTubewwPDB FoundationwwPDBDonate
RCSB PDBPDBeBMRBAdv. SearchSearch help

4BW5

Crystal structure of human two pore domain potassium ion channel TREK2 (K2P10.1)

Summary for 4BW5
Entry DOI10.2210/pdb4bw5/pdb
DescriptorPOTASSIUM CHANNEL SUBFAMILY K MEMBER 10, POTASSIUM ION, CADMIUM ION, ... (4 entities in total)
Functional Keywordstransport protein, outward rectification, membrane protein, k2p
Biological sourceHOMO SAPIENS (HUMAN)
Total number of polymer chains4
Total formula weight126358.34
Authors
Primary citationPike, A.C.W.,Mackenzie, A.,Mcclenaghan, C.,Aryal, P.,Dong, L.,Quigley, A.,Grieben, M.,Goubin, S.,Mukhopadhyay, S.,Ruda, G.F.,Clausen, M.V.,Cao, L.,Brennan, P.E.,Burgess-Brown, N.A.,Sansom, M.S.P.,Tucker, S.J.,Carpenter, E.P.
K2P Channel Gating Mechanisms Revealed by Structures of Trek-2 and a Complex with Prozac
Science, 347:1256-, 2015
Cited by
PubMed 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 intramembrane fenestrations found in only one of these two conformations. Channel activation by arachidonic acid and mechanical stretch involves conversion between these states through movement of the pore-lining helices. These results provide an explanation for TREK channel mechanosensitivity, regulation by diverse stimuli, and possible off-target effects of the serotonin reuptake inhibitor Prozac.
PubMed: 25766236
DOI: 10.1126/SCIENCE.1261512
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (3.2 Å)
Structure validation

239149

數據於2025-07-23公開中

PDB statisticsPDBj update infoContact PDBjnumon