BRET-based effector membrane translocation assay monitors GPCR-promoted and endocytosis-mediated G_q activation at early endosomes.

ABSTRACT: G protein-coupled receptors (GPCRs) are gatekeepers of cellular homeostasis and the targets of a large proportion of drugs. In addition to their signaling activity at the plasma membrane, it has been proposed that their actions may result from translocation and activation of G proteins at endomembranes-namely endosomes. This could have a significant impact on our understanding of how signals from GPCR-targeting drugs are propagated within the cell. However, little is known about the mechanisms that drive G protein movement and activation in subcellular compartments. Using bioluminescence resonance energy transfer (BRET)-based effector membrane translocation assays, we dissected the mechanisms underlying endosomal G_q trafficking and activity following activation of G_q-

SUBMITTER: Wright SC 

PROVIDER: S-EPMC8157916 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature