Direct Detection of RGS GAP Activity Using the RGScreen™ Platform to Discover Small Molecule Inhibitors for RGS Proteins

Transcreener® is a universal, high throughput biochemical assay platform based on the detection of nucleotides, which are formed by thousands of cellular enzymes—many of which catalyze the covalent regulatory reactions that are central to cell signaling and are of great value as targets in drug discovery. The RGScreen Platform uses proprietary Ga protein variants with altered GTP hydrolysis and GDP dissociation rates that enable detection of RGS protein GAP activity by the Transcreener GDP Assay.