Application Note: Monitoring functional inhibition of a cell surface receptor using RNA interference
15 October 2008

This bulletin describes a straightforward and effective method for monitoring functional knockdown of an endogenous cell surface receptor using the CellKeysup™ System and transiently transfected small interfering ribonucleic acids (siRNAs).

The CellKeysup™ System is a label-free, cell-based assay platform that enables comprehensive pharmacological evaluation of cell surface receptors. RNA interference (RNAi) has been rapidly adopted as a useful tool for key drug discovery tasks including target identification and validation, compound selectivity, and mechanism of action (MOA) studies. The CellKeysup™ System measures an integrated cellular response to receptor activation in a non-invasive manner providing an ideal platform to analyze functional knockdown of receptors and other key targets for signaling pathway analyses. Knockdown of receptor function can be monitored sequentially over time on the same set of live, intact cells. Transfections and assays can also be performed directly in the same CellKeysup™ Standard 96W microplate. These features help streamline the process of using RNAi as a tool in the drug discovery process, saving time and cost.