Research progress in regulators of G-protein signaling as new central nervous system drug targets / 中国药理学通报

ABSTRACT

G-protein-coupled receptors (GPCRs) are major targets for drug discovery. The regulator of G-protein signaling (RGS) proteins is a recently identified protein family,which strongly modulates the activity of G proteins. RGS proteins accelerate the deactivation of G proteins to reduce GPCR signaling; however, some also have an effector function and transmit signals. Combining GPCR agonists with RGS inhibitors should potentiate responses and markedly increase the regional specificity of agonist. In the central nervous system, RGS proteins have unique tissue distributions and are strongly regulated by signal transduction events. Thus the diversity of RGS makes them attractive targets for pharmacotherapy of neurological disorders.