Regulators of G-Protein signalling as new central nervous system drug targets
- 1 March 2002
- journal article
- review article
- Published by Springer Science and Business Media LLC in Nature Reviews Drug Discovery
- Vol. 1 (3), 187-197
- https://doi.org/10.1038/nrd747
Abstract
G-protein-coupled receptors (GPCRs) are major targets for drug discovery. The regulator of G-protein signalling (RGS)-protein family has important roles in GPCR signal transduction. RGS proteins contain a conserved RGS-box, which is often accompanied by other signalling regulatory elements. RGS proteins accelerate the deactivation of G proteins to reduce GPCR signalling; however, some also have an effector function and transmit signals. Combining GPCR agonists with RGS inhibitors should potentiate responses, and could markedly increase the agonist's regional specificity. The diversity of RGS proteins with highly localized and dynamically regulated distributions in brain makes them attractive targets for pharmacotherapy of central nervous system disorders.Keywords
This publication has 85 references indexed in Scilit:
- Lifetime Regulation of G Protein–Effector Complex: Emerging Importance of RGS ProteinsNeuron, 1998
- RGS10 is a selective activator of Gαi GTPase activityNature, 1996
- RGS family members: GTPase-activating proteins for heterotrimeric G-protein α-subunitsNature, 1996
- GAIP and RGS4 Are GTPase-Activating Proteins for the Gi Subfamily of G Protein α SubunitsCell, 1996
- A new family of regulators of G-protein-coupled receptors?Current Biology, 1996
- Inhibition of G-protein-mediated MAP kinase activation by a new mammalian gene familyNature, 1996
- EGL-10 Regulates G Protein Signaling in the C. elegans Nervous System and Shares a Conserved Domain with Many Mammalian ProteinsCell, 1996
- GAIP, a protein that specifically interacts with the trimeric G protein G alpha i3, is a member of a protein family with a highly conserved core domain.Proceedings of the National Academy of Sciences of the United States of America, 1995
- G PROTEINS: TRANSDUCERS OF RECEPTOR-GENERATED SIGNALSAnnual Review of Biochemistry, 1987
- Isolation and genetic analysis of Saccharomyces cerevisiae mutants supersensitive to G1 arrest by a factor and alpha factor pheromones.Molecular and Cellular Biology, 1982