Target intelligence / Profile preview

Estrogen-related receptor alpha (ERRα)

Target
ERRα
Molecular classification
Nuclear hormone receptor, Transcription factor, Orphan nuclear receptor
01

Overview

Estrogen-related receptor alpha (ERRα), also known as ESRRA or NR3B1, is an orphan nuclear receptor that plays a central role in regulating cellular metabolism, particularly in tissues with high energy demands such as cardiac and skeletal muscle. Despite its structural similarity to classical estrogen receptors, ERRα does not bind estrogens with high affinity and has no well-established endogenous ligand. ERRα acts primarily as a transcription factor, binding specific DNA sequences to regulate genes involved in mitochondrial biogenesis, oxidative phosphorylation, and fatty acid oxidation. It is predominantly expressed in metabolically active tissues like the heart, skeletal muscle, and brown adipose tissue and is implicated in diseases such as cancer, insulin resistance, and NAFLD.

Other names
ESRRANR3B1
02

Mechanism of action

Binds to specific DNA sequences (TNAAGGTCA) to regulate gene expression; interacts with PGC-1α to enhance mitochondrial function and metabolic regulation.

03

Biological functions

Transcriptional regulationMitochondrial biogenesisOxidative phosphorylation regulationFatty acid oxidation regulationAutophagy regulationMitophagy regulationGene expression regulationSteroidogenesis (in adrenal cells)
04

Disease associations

Cancer (breast, ovarian)Insulin resistanceMetabolic disordersNon-alcoholic fatty liver disease (NAFLD)

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