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Gq-mER

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The Gq-coupled membrane estrogen receptor (Gq-mER) is a G protein-coupled receptor present in the hypothalamus that has not yet been cloned. It is a membrane-associated receptor that is Gq-coupled to a phospholipase Cprotein kinase Cprotein kinase A (PLC–PKC–PKA) pathway. The receptor has been implicated in the control of energy homeostasis. Gq-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 Gq-mER, but is not selective.

See also

References

  1. ^ 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. ^ 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. ^ 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.
Cell surface receptor: G protein-coupled receptors
Class A: Rhodopsin-like
Neurotransmitter
Adrenergic
Purinergic
Serotonin
Other
Metabolites and
signaling molecules
Eicosanoid
Other
Peptide
Neuropeptide
Other
Miscellaneous
Taste, bitter
Orphan
Other
Class B: Secretin-like
Adhesion
Orphan
Other
Class C: Metabotropic glutamate / pheromone
Taste, sweet
Other
Class F: Frizzled & Smoothened
Frizzled
Smoothened
Estrogen receptor modulators
ERTooltip Estrogen receptor
Agonists
Mixed
(SERMsTooltip Selective estrogen receptor modulators)
Antagonists
  • Coregulator-binding modulators: ERX-11
GPERTooltip G protein-coupled estrogen receptor
Agonists
Antagonists
Unknown
See also
Receptor/signaling modulators
Estrogens and antiestrogens
Androgen receptor modulators
Progesterone receptor modulators
List of estrogens
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