Target intelligence / Profile preview

Estrogen receptor (ER)

Target
ER
Molecular classification
Receptor, Nuclear hormone receptor, Transcription factor
01

Overview

The estrogen receptor (ER) is a nuclear hormone receptor and ligand-activated transcription factor found in many tissues, including breast tissue. In breast cancer, ER-positive tumors are defined by the presence of estrogen receptors on tumor cell nuclei and depend on estrogen for proliferation and growth. These receptors bind estrogen, inducing a conformational change that allows them to regulate the transcription of target genes involved in cell proliferation and survival. Roughly 70-80% of all breast cancers are ER-positive, making ER the most common and extensively validated therapeutic target in breast cancer. Therapeutic inhibitors—either by blocking the receptor (SERMs, SERDs) or reducing estrogen production (aromatase inhibitors)—can effectively limit tumor growth. The testing for ER expression is critical in breast cancer diagnosis, prognosis, and treatment planning, and is usually performed using immunohistochemistry on tumor tissue. ER status also guides the use of hormone therapies and predicts the benefit from these treatments.

Other names
Estrogen receptorEREstrogen receptor alpha (ERα)Estrogen receptor beta (ERβ)ESR1Hormone receptor
02

Mechanism of action

Selective estrogen receptor modulators (SERMs): bind to ER, block estrogen signaling in breast tissue (e.g., tamoxifen). Selective estrogen receptor degraders (SERDs): promote degradation of the estrogen receptor (e.g., fulvestrant). Aromatase inhibitors: decrease estrogen synthesis, lowering ligand availability for the receptor.

03

Biological functions

Hormone signalingGene transcription regulationCell proliferationCell growthTumor progression
04

Disease associations

Cancer (especially breast cancer, endometrial cancer, others)Hormone-dependent tumorigenesisOther estrogen-mediated disorders
05

Safety considerations

Risk of resistance to endocrine (hormone) therapyHormonal therapy adverse effects: thromboembolic events, endometrial cancer (tamoxifen), bone loss or fractures (aromatase inhibitors), menopausal symptoms
06

Interacting drugs

Tamoxifen

6 more in the full profile.

07

Biomarkers

Estrogen receptor (ER/ERα) protein expression (by immunohistochemistry/IHC)Progesterone receptor (PR) expressionKi-67 proliferation index (prognostic)Sometimes HER2 status as part of integrated molecular classificationESR1 gene mutations (in resistance)

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