The goal of the present study was to investigate a possible role for regulators of G protein-signaling (RGS) proteins in opioid receptor (OR) desensitization using cultured Xenopus laevis dermal melanophores. Morphine-induced pigment aggregation in a melanophore cell line stably expressing the murine mu OR (muOR) was quantified over time. Responses of the muOR (a G(i)-linked receptor) exhibited...

AIMS Regulator of G protein signalling (RGS) proteins act as molecular 'off switches' that terminate G protein signalling by catalyzing the hydrolysis of Gα-bound GTP to GDP. Many different Gα(i)-coupled receptors have been implicated in the cardioprotective effects of ischaemic preconditioning. However, the role of RGS proteins in modulating cardioprotection has not been previously investigate...

The Randomized Gauss-Seidel Method (RGS) is an iterative algorithm that solves overdetermined systems of linear equations Ax = b. This paper studies an update on the RGS method, the Randomized Block Gauss-Seidel Method(RBGS). At each step, the algorithm greedily minimizes the objective function L(x) = kAx bk2 with respect to a subset of coordinates. This paper describes a Randomized Block Gauss...

G-Protein–coupled receptors (GPCRs) are involved in the regulation of virtually every physiological process. These receptors operate by catalyzing the GDP/GTP exchange at a coupled heterotrimeric G protein (G ), thereby promoting the dissociation of the heterotrimer into a free GTP-liganded G -subunit and a G dimer. Both G and G -dimer then regulate the activity of effectors, eg, secondmessenge...

Because G-protein coupled receptors (GPCRs) continue to represent excellent targets for the discovery and development of small-molecule therapeutics, it is posited that additional protein components of the signal transduction pathways emanating from activated GPCRs themselves are attractive as drug discovery targets. This review considers the drug discovery potential of two such components: mem...

Presynaptic inhibition mediated by G protein-coupled receptors (GPCRs) can develop and decay in a few seconds. This time course is too rapid to be accounted for by the intrinsic GTPase activity of Galpha subunits alone. Here, we test the hypothesis that endogenous regulators of G protein signaling (RGS proteins) are required for rapid, brief presynaptic inhibition. Endogenous G protein alpha su...

RGS14 is a 60 kDa protein that contains a regulator of G protein signaling (RGS) domain near its N-terminus, a central region containing a pair of tandem Ras-binding domains (RBD), and a GPSM (G protein signaling modulator) domain (a.k.a. Gi/o-Loco binding [GoLoco] motif) near its C-terminus. The RGS domain of RGS14 exhibits GTPase accelerating protein (GAP) activity toward Gαi/o proteins, whil...

Background: Gb proteins have traditionally been thought to complex with Address: Department of Molecular Biophysics and Biochemistry, Yale University, New Haven, Gg proteins to function as subunits of G protein heterotrimers. The Connecticut 06520, USA. divergent Gb5 protein, however, can bind either Gg proteins or regulator of G protein signaling (RGS) proteins that contain a G gamma–like (GGL...

Regulators of G-protein signaling (RGS) proteins are known for the RGS domain that is composed of a conserved stretch of 120 amino acids, which binds directly to activated G-protein alpha subunits and acts as a GTPase-activating protein (GAP), leading to their deactivation and termination of downstream signals. In this study, a novel human RGS cDNA (RGS21), 1795 bp long and encoding a 152-amino...

Regulator of G protein signaling (RGS) proteins accelerate the endogenous GTPase activity of Galpha(i/o) proteins to increase the rate of deactivation of active Galpha-GTP and Gbetagamma signaling molecules. Previous studies have suggested that RGS proteins are more effective on less efficiently coupled systems such as with partial agonist responses. To determine the role of endogenous RGS prot...