RGS17
Description
The RGS17 (regulator of G protein signaling 17) is a protein-coding gene located on chromosome 6.
RGS17, or Regulator of G-protein signaling 17, is a protein encoded by the RGS17 gene in humans. It belongs to the regulator of G-protein signaling family, characterized by a conserved 120 amino acid motif called the RGS domain and a cysteine-rich region. RGS17 dampens the signaling activity of G-proteins by binding to activated, GTP-bound G alpha subunits and acting as a GTPase activating protein (GAP), accelerating the conversion of GTP to GDP. This hydrolysis facilitates the binding of G alpha subunits to G beta/gamma subunit heterodimers, forming inactive G-protein heterotrimers, ultimately terminating the signal. RGS17, along with RGS4, RGS9, and RGS14, plays a crucial role in terminating signaling by mu opioid receptors and the development of tolerance to opioid analgesic drugs. RGS17 is a potential lung cancer susceptibility gene located within the lung cancer associated locus on chromosome 6q. It is overexpressed in lung and prostate cancers, stimulating cAMP production, CREB phosphorylation, and CREB responsive gene expression. Furthermore, expression of RGS17 is required for maintaining proliferation in lung tumor cell lines.
RGS17 modulates G protein-coupled receptor signaling pathways, including those triggered by muscarinic acetylcholine receptor CHRM2 and dopamine receptor DRD2. It dampens signal transmission by enhancing the GTPase activity of G protein alpha subunits, ultimately shifting them to their inactive GDP-bound state. RGS17 exhibits preferential binding to GNAZ and GNAI2 subunits, accelerating their GTPase activity and influencing their signaling actions. Additionally, RGS17 negatively regulates mu-opioid receptor-mediated activation of G-proteins.
RGS17 is also known as RGS-17, RGSZ2, hRGS17.
