RGS Protein GAP Assays

• Universal RGS Protein Detection: The only HTS-ready assay method for RGS GAP activity
• A Complete Screening and Profiling Solution: Recombinant Proteins RGS proteins, kinetically enhanced Gα proteins, and Transcreener GDP Assay detection reagents.

Members of the "regulator of G-protein signaling" (RGS)-protein superfumily act as "GTPase-accelerating proteins" (GAP) for heterotrimeric G-protein alpha subunits, thereby attenuating GPCR signaling. Their selectivity for specific GPCRs and downstream signaling components and their tissue- specific expression makes them attractive as potential therapeutic targets, with the potential for modulating the effects of existing GPCR agonists.

RGScreen: The only HTS assay for RGS Protein GAP Activity

The most direct way to detect RGS function is by measuring the increased GTPase activity of the associated Gα protein. However, the GTPase activity of isolated Gα proteins is limited by GDP dissociation, so RGS GAP activity cannot be measured using simple biochemical assays. The RGScreen platform overcomes this kinetic constraint by using proprietary Gα protein variants with altered GTP hydrolysis and GDP dissociation rates that enable detection of RGS GAP activity using the Transcreener® GDP Assay.

Recombinant RGS Proteins and Kinetically Enhanced Gα Proteins

(Quantities of each protein vary; sufficient protein for 1,000 assays in 384-well format.)

Transcreener GDP Assay