Intracellular regulation of heterotrimeric G-protein signaling in normal and diseased tissues of the cardiovascular system

Excessive G-protein coupled receptor (GPCR) signaling can promote pathogenesis of cardiovascular disease. Thus, much work has been carried out to identify the molecular pathways modulating GPCR signaling in cardiovascular tissues. Herein, one such family of GPCR modulators is described in detail. Specifically, this work focuses on the RGS superfamily of proteins, with emphasis on the genetic models that have been used to understand their biologic roles in cardiovascular tissues. Whereas some RGS family members inhibit GPCR pathways, others behave as effectors of GPCR signaling. Therefore, to evaluate the therapeutic potential of targeting RGS proteins, one needs to understand the GPCR pathways it regulates, and its role as either an inhibitor or activator of signaling. Lastly, this work discusses the current state of development of pharmacologic modulators of RGS protein activity in the context of their therapeutic potential.