Regulator of G protein signaling (RGS) proteins represent unique targets for the modulation of G protein-coupled receptor-mediated signal transduction cascades. Functionally, RGS proteins act to limit the duration of signaling of activated G proteins due to its ability to act as GTPase activating proteins (GAPs). This GAP activity catalyzes the intrinsic GTPase activity of G protein α subunits, such as those in the Gαo, Gαi, and Gαq families. Because of their unique regulatory properties, RGS proteins have emerged as an interesting target for development of both small molecule laboratory tools and potential future therapeutics. In this chapter, the utility of RGS modulators will be briefly reviewed, with a main focus on high-throughput screening methods and progress being made to discover new RGS ligands.
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