Identification and characterization of novel PAM's of the Galanin 2 receptor
As a result the galanin system, and specifically the galanin 2 receptor (GalR2) has been identified as a potential target for novel therapeutics.
In BMG LABTECH application note 236 the authors describe the screening procedure used to identify positive allosteric modulators of GalR2 using the PHERAstar microplate reader.
In the application note the authors exploit the fact that GalR2 is a G-protein coupled receptor and used the HTRF IP1 assay from Cisbio as a read out of the activity of this receptor. Using this assay a high throughput screen was performed which was simplified by the availability of an HTRF optic module for the PHERAstar from BMG LABTECH. The screen exhibited strong statistical results which indicate that the approach employed is indeed suitable for high through put and can be used for additional screening as necessary.
For more information on the PHERAstar and other microplate readers click on the links.