Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs
Institute for Research in Immunology and Cancer · Université de Montréal · +3 more institutions
Abstract
The recognition that individual GPCRs can activate multiple signaling pathways has raised the possibility of developing drugs selectively targeting therapeutically relevant ones. This requires tools to determine which G proteins and βarrestins are activated by a given receptor. Here, we present a set of BRET sensors monitoring the activation of the 12 G protein subtypes based on the translocation of their effectors to the plasma membrane (EMTA). Unlike most of the existing detection systems, EMTA does not require modification of receptors or G proteins (except for G s ). EMTA was found to be suitable for the detection of constitutive activity, inverse agonism, biased signaling and polypharmacology. Profiling…
Citation impact
- FWCI
- 19.75
- Percentile
- 100%
- References
- 62
Authors
20- CACharlotte AvetCorresponding
Institute for Research in Immunology and Cancer, Université de Montréal
- AMArturo Mancini
Domain Therapeutics (France)
- BBBilly Breton
Domain Therapeutics (France)
- CLChristian Le Gouill
Institute for Research in Immunology and Cancer, Université de Montréal
- ASAlexander S. Hauser
University of Copenhagen
Topics & keywords
- G protein-coupled receptor
- Effector
- Arrestin
- Chromosomal translocation
- Cell biology
- Computational biology
- Biology
- Membrane protein