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 discovery targeting G protein-coupled receptors (GPCRs) is no longer limited to
seeking agonists or antagonists to stimulate or block cellular responses associated with a …

Drug discovery efforts targeting G-protein-coupled receptors (GPCR) have been immensely
successful in creating new cardiovascular medicines. Currently marketed GPCR drugs are …

Many proteins associated with the plasma membrane are known to partition into submicroscopic
sphingolipid- and cholesterol-rich domains called lipid rafts, but the determinants …

For many years, β-adrenergic receptor antagonists (β-blockers or βAR antagonists) have
provided significant morbidity and mortality benefits in patients who have sustained acute …

The concept of ligand bias at G protein-coupled receptors broadens the possibilities for
agonist activities and provides the opportunity to develop safer, more selective therapeutics. …

Signals transduced by kinases depend on the extent and duration of substrate phosphorylation.
We generated genetically encoded fluorescent reporters for PKC activity that reversibly …

Acute stimulation of cardiac β1-adrenergic receptors (β1ARs) by norepinephrine represents
the strongest endogenous mechanism for increasing cardiac function, but long-term …

Classically, the β 2 -adrenergic receptor (β 2 AR) and other members of the seven-transmembrane
receptor (7TMR) superfamily activate G protein-dependent signaling pathways in …

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 …