CONTEXT

TREK-1 potassium channels are involved in a number of physiopathological processes such as neuroprotection, pain and depression. Molecules able to open or to block these channels can be clinically important. Having a cell model for screening such molecules is of particular interest. 

TECHNICAL DESCRIPTION

The inventors have developed the first available cell line that constitutively expresses the TREK-1 channel.
This cell line has been fully characterized with regards to the modulation properties of the TREK-1 channel that is expressed. The results show that all its properties are retained: it is opened by stretch, pH, polyunsaturated fatty acids and by the neuroprotective molecule, riluzole and it is blocked by spadin or fluoxetine. In addition, the inventors have also demonstrated that the h-TREK-1/HEK cell line is protected against ischemia by using the oxygen-glucose deprivation model.

A) Typical pictures of cells observed in transmission and in fluorescence at round three of cell culture. Functional channel activity was evaluated by current activation with 10 µM AA.
B) Typical pictures of cells observed in transmission and in fluorescence at round fourteenth of cell culture. Functional channel activity was evaluated by current activation with 10 µM AA.
C) Real time q-PCR. Levels of TREK-1 or sortilin expression were normalized with the cyclophillin D expression.

INDUSTRIAL APPLICATIONS

High Throughput Screening on the TREK-1 target for drug discovery.

PUBLICATIONS

A human TREK-1/HEK cell line: a highly efficient screening tool for drug development in neurological diseases.
Moha ou Maati H et al. PLoS One. 2011;6(10):e25602.

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