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Gq-mER

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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. ^ a b c d e Qiu, J. (2006). "A G-Protein-Coupled Estrogen Receptor Is Involved in Hypothalamic Control of Energy Homeostasis". Journal of Neuroscience. 26 (21): 5649–5655. doi:10.1523/JNEUROSCI.0327-06.2006. ISSN 0270-6474. PMC 2678732. PMID 16723521.
  2. ^ a b c d Laredo, Sarah A.; Villalon Landeros, Rosalina; Trainor, Brian C. (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. ISSN 0091-3022.
  3. ^ a b Micevych, Paul E.; Kelly, Martin J. (2012). "Membrane Estrogen Receptor Regulation of Hypothalamic Function". Neuroendocrinology. 96 (2): 103–110. doi:10.1159/000338400. ISSN 1423-0194. PMC 3496782. PMID 22538318.


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