Target intelligence / Profile preview

Estrogen-related receptor gamma (ERRγ)

Target
ERRγ
Molecular classification
Nuclear hormone receptor, Steroid hormone receptor, Transcription factor
01

Overview

Estrogen-related receptor gamma (ERRγ) is a nuclear receptor that functions as a constitutive activator of transcription. It plays a crucial role in regulating oxidative metabolism and angiogenesis. While no endogenous activating ligand has been identified, ERRγ can be modulated by inverse agonists like 4-hydroxytamoxifen and diethylstilbestrol, and by xenoestrogens like Bisphenol A (BPA). ERRγ is implicated in various diseases, including breast cancer, endometrial cancer, metabolic disorders, and cardiovascular diseases, making it an attractive target for drug development.

Other names
NR3B3ESRRG
02

Mechanism of action

Constitutive activation of transcription; Modulation via inverse agonists and xenoestrogens.

03

Biological functions

Transcriptional activationRegulation of oxidative metabolismRegulation of angiogenesis
04

Disease associations

Breast cancerEndometrial cancerMetabolic disordersCardiovascular diseases
05

Safety considerations

Potential for endocrine disruption due to interactions with environmental chemicals like BPA.Off-target effects due to structural similarity with other estrogen-related receptors.
06

Interacting drugs

4-hydroxytamoxifen

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