Biology:Gq-mER

From HandWiki

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]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "A G-protein-coupled estrogen receptor is involved in hypothalamic control of energy homeostasis". The Journal of Neuroscience 26 (21): 5649–5655. May 2006. doi:10.1523/JNEUROSCI.0327-06.2006. PMID 16723521. 
  2. ↑ 2.0 2.1 2.2 2.3 "Rapid effects of estrogens on behavior: environmental modulation and molecular mechanisms". Frontiers in Neuroendocrinology 35 (4): 447–458. October 2014. doi:10.1016/j.yfrne.2014.03.005. PMID 24685383. 
  3. ↑ 3.0 3.1 "Membrane estrogen receptor regulation of hypothalamic function". Neuroendocrinology 96 (2): 103–110. 2012. doi:10.1159/000338400. PMID 22538318. 



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