G-protein–coupled receptors in heart disease
GPCRs (G-protein [guanine nucleotide-binding protein]–coupled receptors) play a central
physiological role in the regulation of cardiac function in both health and disease and thus …
physiological role in the regulation of cardiac function in both health and disease and thus …
The diverse roles of arrestin scaffolds in G protein–coupled receptor signaling
YK Peterson, LM Luttrell - Pharmacological reviews, 2017 - ASPET
The visual/β-arrestins, a small family of proteins originally described for their role in the
desensitization and intracellular trafficking of G protein–coupled receptors (GPCRs), have …
desensitization and intracellular trafficking of G protein–coupled receptors (GPCRs), have …
Biased receptor signaling in drug discovery
T Kenakin - Pharmacological reviews, 2019 - ASPET
A great deal of experimental evidence suggests that ligands can stabilize different receptor
active states that go on to interact with cellular signaling proteins to form a range of different …
active states that go on to interact with cellular signaling proteins to form a range of different …
Manifold roles of β-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9
G protein–coupled receptors (GPCRs) use diverse mechanisms to regulate the mitogen-
activated protein kinases ERK1/2. β-Arrestins (βArr1/2) are ubiquitous inhibitors of G protein …
activated protein kinases ERK1/2. β-Arrestins (βArr1/2) are ubiquitous inhibitors of G protein …
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 …
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 …
G protein–coupled receptor signaling through β-arrestin–dependent mechanisms
PY Jean-Charles, S Kaur… - Journal of cardiovascular …, 2017 - journals.lww.com
β-arrestin1 (or arrestin2) and β-arrestin2 (or arrestin3) are ubiquitously expressed cytosolic
adaptor proteins that were originally discovered for their inhibitory role in G protein–coupled …
adaptor proteins that were originally discovered for their inhibitory role in G protein–coupled …
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 …
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) …
Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance
JD Violin, SM DeWire, D Yamashita… - … of Pharmacology and …, 2010 - ASPET
Biased G protein-coupled receptor ligands engage subsets of the receptor signals normally
stimulated by unbiased agonists. However, it is unclear whether ligand bias can elicit …
stimulated by unbiased agonists. However, it is unclear whether ligand bias can elicit …