[HTML][HTML] Quantitative phosphoproteomics dissection of seven-transmembrane receptor signaling using full and biased agonists

GL Christensen, CD Kelstrup, C Lyngsø… - Molecular & cellular …, 2010 - ASBMB
Seven-transmembrane receptors (7TMRs) signal through the well described heterotrimeric
G proteins but can also activate G protein-independent signaling pathways of which the
impact and complexity are less understood. The angiotensin II type 1 receptor (AT 1 R) is a
prototypical 7TMR and an important drug target in cardiovascular diseases." Biased
agonists" with intrinsic" functional selectivity" that simultaneously blocks Gα q protein activity
and activates G protein-independent pathways of the AT 1 R confer important perspectives …