[HTML][HTML] Heterotrimeric G proteins directly regulate MMP14/membrane type-1 matrix metalloprotease: a novel mechanism for GPCR-EGFR transactivation

AC Overland, PA Insel - Journal of Biological Chemistry, 2015 - ASBMB
Agonist stimulation of G protein-coupled receptors (GPCRs) can transactivate epidermal
growth factor receptors (EGFRs), but the precise mechanisms for this transactivation have
not been defined. Key to this process is the protease-mediated" shedding" of membrane-
tethered ligands, which then activate EGFRs. The specific proteases and the events involved
in GPCR-EGFR transactivation are not fully understood. We have tested the hypothesis that
transactivation can occur by a membrane-delimited process: direct increase in the activity of …