Rapid Selection and Development of GPCR Expressing Mammalian Cell lines using Novel ClonePix Technology
11 November 2015

The endogenous expression of G protein-coupled receptors (GPCRs) in mammalian cells is typically very low, generally with no more than 3,000 copies per cell. These endogenous expression levels are sufficient to maintain proper receptor function but present a challenge with respect to GPCR drug discovery efforts. For example, structural studies, small molecule drug design and generation of functional antibodies against native GPCR targets require expression levels that are orders of magnitude higher than endogenous levels. Attempts to create expression systems in “lower” organisms have met with limited success due to inefficient folding (bacteria), low yield (yeast) or incorrect post-translation modification (baculovirus). These challenges fuel the market need for mammalian expression systems capable of providing the elevated GPCR protein expression levels required to support drug discovery efforts. This application note demonstrates the feasibility of using the ClonePix 2 System to detect cell surface expressed proteins.