Gq-mER explained

The G_q-coupled membrane estrogen receptor (G_q-mER) is a G protein-coupled receptor present in the hypothalamus that has not yet been cloned.^{[1] [2]} It is a membrane-associated receptor that is G_q-coupled to a phospholipase C–protein kinase C–protein kinase A (PLC–PKC–PKA) pathway. The receptor has been implicated in the control of energy homeostasis.^[1] G_q-mER is bound and activated by estradiol, and is a putative membrane estrogen receptor (mER). A nonsteroidal diphenylacrylamide derivative, STX, which is structurally related to 4-hydroxytamoxifen (afimoxifene), is an agonist of the receptor with greater potency than estradiol (20-fold higher affinity) that has been discovered. Fulvestrant (ICI-182,780) has been identified as an antagonist of G_q-mER, but is not selective.^[3]

See also

• Estrogen receptor
• GPER (GPR30)
• ER-X
• ERx

Notes and References

1. Qiu J, Bosch MA, Tobias SC, Krust A, Graham SM, Murphy SJ, Korach KS, Chambon P, Scanlan TS, Rønnekleiv OK, Kelly MJ . 6 . A G-protein-coupled estrogen receptor is involved in hypothalamic control of energy homeostasis . The Journal of Neuroscience . 26 . 21 . 5649–5655 . May 2006 . 16723521 . 2678732 . 10.1523/JNEUROSCI.0327-06.2006 .
2. Laredo SA, Villalon Landeros R, Trainor BC . Rapid effects of estrogens on behavior: environmental modulation and molecular mechanisms . Frontiers in Neuroendocrinology . 35 . 4 . 447–458 . October 2014 . 24685383 . 4175137 . 10.1016/j.yfrne.2014.03.005 .
3. Micevych PE, Kelly MJ . Membrane estrogen receptor regulation of hypothalamic function . Neuroendocrinology . 96 . 2 . 103–110 . 2012 . 22538318 . 3496782 . 10.1159/000338400 .