Therapeutic potential of β-arrestin-and G protein-biased agonists

EJ Whalen, S Rajagopal, RJ Lefkowitz - Trends in molecular medicine, 2011 - cell.com
Members of the seven-transmembrane receptor (7TMR), or G protein-coupled receptor
(GPCR), superfamily represent some of the most successful targets of modern drug therapy …

β-Arrestin-biased ligands at seven-transmembrane receptors

JD Violin, RJ Lefkowitz - Trends in pharmacological sciences, 2007 - cell.com
Seven-transmembrane receptors (7TMRs), the most common molecular targets of modern
drug therapy, are critically regulated by β-arrestins, which both inhibit classic G-protein …

Teaching old receptors new tricks: biasing seven-transmembrane receptors

S Rajagopal, K Rajagopal, RJ Lefkowitz - Nature reviews Drug …, 2010 - nature.com
Abstract Seven-transmembrane receptors (7TMRs; also known as G protein-coupled
receptors) are the largest class of receptors in the human genome and are common targets …

β‐arrestins and heterotrimeric G‐proteins: collaborators and competitors in signal transduction

K Defea - British journal of pharmacology, 2008 - Wiley Online Library
G‐protein‐coupled receptors (GPCRs), also known as seven transmembrane receptors (7‐
TMRs), are the largest protein receptor superfamily in the body. These receptors and their …

Emerging paradigms of β-arrestin-dependent seven transmembrane receptor signaling

AK Shukla, K Xiao, RJ Lefkowitz - Trends in biochemical sciences, 2011 - cell.com
β-Arrestins, originally discovered to desensitize activated seven transmembrane receptors
(7TMRs; also known as G-protein-coupled receptors, GPCRs), are now well established …

Molecular mechanism of β-arrestin-biased agonism at seven-transmembrane receptors

E Reiter, S Ahn, AK Shukla… - Annual review of …, 2012 - annualreviews.org
The concept of biased agonism has recently come to the fore with the realization that seven-
transmembrane receptors (7TMRs, also known as G protein–coupled receptors, or GPCRs) …

Distinct conformational changes in β-arrestin report biased agonism at seven-transmembrane receptors

AK Shukla, JD Violin, EJ Whalen… - Proceedings of the …, 2008 - National Acad Sciences
β-arrestins critically regulate G protein-coupled receptors (GPCRs), also known as seven-
transmembrane receptors (7TMRs), both by inhibiting classical G protein signaling and by …

β-Arrestin-mediated receptor trafficking and signal transduction

SK Shenoy, RJ Lefkowitz - Trends in pharmacological sciences, 2011 - cell.com
β-Arrestins function as endocytic adaptors and mediate trafficking of a variety of cell-surface
receptors, including seven-transmembrane receptors (7TMRs). In the case of 7TMRs, β …

[HTML][HTML] Seven-transmembrane receptor signaling through β-arrestin

SK Shenoy, RJ Lefkowitz - Science's STKE, 2005 - science.org
Cell surface receptors are important communicators of external stimuli to the cell interior
where they lead to initiation of various signaling pathways and cellular responses. The …

Physiological and pharmacological implications of beta-arrestin regulation

CL Schmid, LM Bohn - Pharmacology & therapeutics, 2009 - Elsevier
G protein-coupled receptor-targeted drug discovery as well as “compound reassessment”
requires the utilization of diverse screens to determine agonist efficacies and potencies …