Regulators of G-protein signaling and their Gα substrates: promises and challenges in their use as drug discovery targets

AJ Kimple, DE Bosch, PM Giguere, DP Siderovski… - Pharmacological …, 2011 - Elsevier
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 …

Isoprenylated proteins

SJ McTaggart - Cellular and Molecular Life Sciences CMLS, 2006 - Springer
Isoprenoids are synthesized in all living organisms and are incorporated into diverse
classes of end-products that participate in a multitude of cellular processes relating to cell …

The role of Gβγ subunits in the organization, assembly, and function of GPCR signaling complexes

DJ Dupré, M Robitaille, RV Rebois… - Annual review of …, 2009 - annualreviews.org
The role of Gβγ subunits in cellular signaling has become well established in the past 20
years. Not only do they regulate effectors once thought to be the sole targets of Gα subunits …

GABAB receptor coupling to G-proteins and ion channels

CL Padgett, PA Slesinger - Advances in pharmacology, 2010 - Elsevier
GABA B receptors have been found to play a key role in regulating membrane excitability
and synaptic transmission in the brain. The GABA B receptor is a G-protein coupled receptor …

Heterotrimeric G proteins precouple with G protein-coupled receptors in living cells

M Nobles, A Benians, A Tinker - Proceedings of the …, 2005 - National Acad Sciences
Using fluorescence resonance energy transfer (FRET) microscopy, we investigate how
heterotrimeric G proteins interact with G protein-coupled receptors (GPCRs). In the absence …

RGS proteins have a signalling complex: interactions between RGS proteins and GPCRs, effectors, and auxiliary proteins

M Abramow-Newerly, AA Roy, C Nunn, P Chidiac - Cellular signalling, 2006 - Elsevier
The intracellular regulator of G protein signalling (RGS) proteins were first identified as
GTPase activating proteins (GAPs) for heterotrimeric G proteins, however, it was later found …

R4 RGS proteins: regulation of G-protein signaling and beyond

G Bansal, KM Druey, Z Xie - Pharmacology & therapeutics, 2007 - Elsevier
The regulators of G-protein signaling (RGS) proteins were initially characterized as inhibitors
of signal transduction cascades initiated by G-protein-coupled receptors (GPCR) because of …

Structural features of the G-protein/GPCR interactions

IS Moreira - Biochimica et Biophysica Acta (BBA)-General Subjects, 2014 - Elsevier
Background The details of the functional interaction between G proteins and the G protein
coupled receptors (GPCRs) have long been subjected to extensive investigations with …

Mammalian RGS proteins: multifunctional regulators of cellular signalling

GB Willars - Seminars in cell & developmental biology, 2006 - Elsevier
Regulators of G-protein signalling (RGS) proteins are a large and diverse family initially
identified as GTPase activating proteins (GAPs) of heterotrimeric G-protein Gα-subunits. At …

Higher-order organization and regulation of adenylyl cyclases

DMF Cooper, AJ Crossthwaite - Trends in pharmacological sciences, 2006 - cell.com
There is increasing awareness of the compartmentalization of cAMP signalling–the means
by which cAMP levels change in discrete domains of the cell with discrete local …