Gq-mER

The Gq-coupled membrane estrogen receptor (Gq-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 Gq-coupled to a phospholipase C–protein kinase C–protein kinase A (PLC–PKC–PKA) pathway.[1][2] The receptor has been implicated in the control of energy homeostasis.[1] Gq-mER is bound and activated by estradiol, and is a putative membrane estrogen receptor (mER).[1][2] 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.[1][2][3] Fulvestrant (ICI-182,780) has been identified as an antagonist of Gq-mER, but is not selective.[3]

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