A hydrophobic barrier deep within the inner pore of the TWIK-1 K2P potassium channel.

Article Details

Citation

Aryal P, Abd-Wahab F, Bucci G, Sansom MS, Tucker SJ

A hydrophobic barrier deep within the inner pore of the TWIK-1 K2P potassium channel.

Nat Commun. 2014 Jul 8;5:4377. doi: 10.1038/ncomms5377.

PubMed ID
25001086 [ View in PubMed
]
Abstract

Recent X-ray crystal structures of the two-pore domain (K2P) family of potassium channels have revealed a unique structural architecture at the point where the cytoplasmic bundle-crossing gate is found in most other tetrameric K(+) channels. However, despite the apparently open nature of the inner pore in the TWIK-1 (K2P1/KCNK1) crystal structure, the reasons underlying its low levels of functional activity remain unclear. In this study, we use a combination of molecular dynamics simulations and functional validation to demonstrate that TWIK-1 possesses a hydrophobic barrier deep within the inner pore, and that stochastic dewetting of this hydrophobic constriction acts as a major barrier to ion conduction. These results not only provide an important insight into the mechanisms which control TWIK-1 channel activity, but also have important implications for our understanding of how ion permeation may be controlled in similar ion channels and pores.

DrugBank Data that Cites this Article

Polypeptides
NameUniProt ID
Potassium channel subfamily K member 1O00180Details