RGS4

Regulator of G protein signaling 4 or RGS4 is a protein which regulates G protein signaling.^[1] A number of studies associate the RGS4 gene with schizophrenia,^[2][3][4][5] while some fail to detect an association.^[6]

RGS4 is also of interest as one of the three main RGS proteins (along with RGS9 and RGS17) involved in terminating signalling by the mu opioid receptor,^[7] and may be important in the development of tolerance to opioid drugs.^{[8][9][10][11][12]}

Regulator of G protein signaling (RGS) family members are regulatory molecules that act as GTPase activating proteins (GAPs) for G alpha subunits of heterotrimeric G proteins. RGS proteins are able to deactivate G protein subunits of the Gi alpha, Go alpha and Gq alpha subtypes. They drive G proteins into their inactive GDP-bound forms. Regulator of G protein signaling 4 belongs to this family. All RGS proteins share a conserved 120-amino acid sequence termed the RGS domain. Regulator of G protein signaling 4 protein is 37% identical to RGS1 and 97% identical to rat Rgs4. This protein negatively regulates signaling upstream or at the level of the heterotrimeric G protein and is localized in the cytoplasm.^[1]

^[13]

Inhibitors

• cyclic peptides ^[14]
• CCG-4986 ^[15]

Interactions

RGS4 has been shown to interact with ERBB3,^[16] GNAQ^[17][18] and COPB2.^[19]

References

Further reading