Regulator of G protein signaling 3 (RGS3) (RGS3)

Regulator of G protein signaling 3 (RGS3) is a member of the RGS family that functions as a GTPase-activating protein (GAP) for G alpha subunits, specifically of the Gi and Gq classes [1]. By accelerating the intrinsic GTPase activity of these subunits, RGS3 effectively terminates signaling from G protein-coupled receptors (GPCRs), thereby acting as a critical negative regulator of signal transduction pathways [1, 2]. In pathological contexts, RGS3 is frequently upregulated in various malignancies, including glioblastoma and pancreatic cancer, where it promotes cell proliferation, migration, and epithelial-mesenchymal transition (EMT) [3, 4]. It also plays a role in cardiovascular conditions such as cardiac hypertrophy and has been implicated in inflammatory responses [5, 6]. While there are currently no FDA-approved drugs specifically targeting RGS3, its mRNA and protein are being investigated as therapeutic targets using RNA interference (RNAi) and antisense oligonucleotides (ASOs) to modulate its expression in disease states [4, 7]. The targeting of RGS3 mRNA represents a strategy to overcome the traditional undruggability of RGS proteins by small molecules, with research indicating that silencing RGS3 can inhibit tumor cell invasion and sensitize cells to other treatments [3, 7].

Other names

RGP3C2PARegulator of G-protein signaling 3

Modulation of G protein-coupled receptor signaling by accelerating the hydrolysis of GTP to GDP on G alpha subunits, specifically of the Gi and Gq families.