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 …
(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 …
drug therapy, are critically regulated by β-arrestins, which both inhibit classic G-protein …
Teaching old receptors new tricks: biasing seven-transmembrane receptors
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 …
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 …
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 …
(7TMRs; also known as G-protein-coupled receptors, GPCRs), are now well established …
Molecular mechanism of β-arrestin-biased agonism at seven-transmembrane receptors
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) …
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 …
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 …
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 …
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 …
requires the utilization of diverse screens to determine agonist efficacies and potencies …