Investigation of Different GTPase Classes with the Transcreener ® GDP Assay

The Transcreener® GDP Assays are single step, homogenous, fluorescent assays for direct detection and screening of GTPases. Available with fluorescence polarization (FP) and fluorescence intensity (FI) readouts, they provide a safe, HTS-compatible alternative to cumbersome radioassay methods and are more sensitive and less subject to interference than colorimetric phosphate detection methods. This application note shows enzyme data for various classes of GTPases. RGScreen uses kinetically altered Gα subunits of heterotrimeric G proteins in combination with the Transcreener® GDP Assay to provide a robust HTS method for identifying inhibitors of RGS protein GAP activity: from initial screen to profiling hits.