Target intelligence / Profile preview

Membrane estrogen receptor (putative, ERx) (ERx)

Target
ERx
Molecular classification
Receptor, Transmembrane receptor
01

Overview

ERx is a putative membrane estrogen receptor identified via its associated gene transcription signature that is induced by estradiol independently of the classical nuclear and membrane estrogen receptors ERα, ERβ, and GPER. It was characterized using a membrane-impermeable estradiol conjugate (E2-BSA), in studies where classic ER antagonists and GPER antagonists were used to dissect out independent pathways. Little is known about the molecular identity, structure, or biological roles of ERx. There is no evidence it is targeted by approved drugs or is a validated therapeutic target. Much of the literature using "ERX" actually refers to ERX-11, a small molecule modulator of ERα function, which is unrelated to ERx as a distinct receptor.

Other names
ER-XMembrane estrogen receptormERERx gene signature
02

Mechanism of action

Estradiol-induced gene transcription through a non-ERα/ERβ/GPER pathway

03

Biological functions

Signal transductionRegulation of gene transcription independently of ERα, ERβ, and GPER
04

Disease associations

Potential roles in breast cancer and hormone signaling; not clinically established
05

Safety considerations

Not applicable; no drugs or therapies targeting ERx

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