Assessment of constitutive activity and internalization of GPR54 (KISS1-R)

M Pampillo, AV Babwah - Methods in enzymology, 2010 - Elsevier
The kisspeptin/GPR54 signaling system positively regulates GnRH secretion, thereby acting
as an important regulator of the hypothalamic–pituitary–gonadal axis. It also negatively
regulates tumor metastases and placental trophoblast invasion. GPR54 is a G q/11-coupled
GPCR and activation by kisspeptin stimulates PIP 2 hydrolysis and inositol phosphate (IP)
formation, Ca 2+ mobilization, arachidonic acid release, and ERK1/2 and p38 MAP kinase
phosphorylation. Recently, we reported that GPR54 displays constitutive activity and …