Functional selectivity profiling of the angiotensin II type 1 receptor using pathway-wide BRET signaling sensors

著者: Yoon Namkung, Christian LeGouill, Sahil Kumar, Yubo Cao, Larissa B. Teixeira, Viktoriya Lukasheva, Jenna Giubilaro, Sarah C. Simões, Jean‐Michel Longpré, Dominic Devost, Terence E. Hébert, Graciela Piñeyro, Richard Leduc, Cláudio M. Costa-Neto, Michel Bouvier, Stéphane A. Laporte - Science Signaling 2018 被引用: 156

and β-arrestin, there are also biases among G protein subtypes. We also demonstrated that biases observed at the receptor and G protein levels propagated to downstream signaling pathways and that these biases could occur through the engagement of different G proteins to activate a common effector. We also used these tools to determine how naturally occurring AT1R variants affected signaling bias. This suite of BRET biosensors provides a useful resource for fingerprinting biased ligands and mutant receptors and for dissecting functional selectivity at various levels of GPCR signaling.