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]
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