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Gq-mER
G
q
-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
G
q
-coupled
to a
phospholipase C
–
protein kinase C
–
protein kinase A
(PLC–PKC–PKA) pathway. The receptor has been implicated in the control of energy
homeostasis
. G
q
-mER is bound and activated by
estradiol
, and is a putative
membrane estrogen receptor
(mER). A
non-steroidal
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 G
q
-mER, but is not selective.
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