Estrogen receptor beta

Estrogen receptor 2 (ER beta)
PDB rendering based on 1hj1.
Available structures PDB Ortholog search: PDBe, RCSB List of PDB id codes 1L2J, 1NDE, 1QKM, 1U3Q, 1U3R, 1U3S, 1U9E, 1X76, 1X78, 1X7B, 1X7J, 1YY4, 1YYE, 1ZAF, 2FSZ, 2GIU, 2I0G, 2JJ3, 2NV7, 2QTU, 2YJD, 2YLY, 2Z4B, 3OLL, 3OLS, 3OMO, 3OMP, 3OMQ, 4J24, 4J26
Identifiers
Symbols	ESR2 ; ER-BETA; ESR-BETA; ESRB; ESTRB; Erb; NR3A2
External IDs	OMIM: 601663 MGI: 109392 HomoloGene: 1100 IUPHAR: 621 ChEMBL: 242 GeneCards: ESR2 Gene
Gene ontology Molecular function • core promoter sequence-specific DNA binding • DNA binding • transcription factor activity, sequence-specific DNA binding • steroid hormone receptor activity • transcription coactivator activity • RNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA binding • steroid binding • protein binding • zinc ion binding • enzyme binding • estrogen receptor activity • estrogen response element binding • receptor antagonist activity Cellular component • extracellular region • nucleus • nucleoplasm • mitochondrion Biological process • negative regulation of transcription from RNA polymerase II promoter • regulation of transcription, DNA-templated • transcription initiation from RNA polymerase II promoter • signal transduction • cell-cell signaling • gene expression • negative regulation of cell growth • intracellular estrogen receptor signaling pathway • steroid hormone mediated signaling pathway • positive regulation of transcription, DNA-templated • positive regulation of sequence-specific DNA binding transcription factor activity • extracellular negative regulation of signal transduction Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	2100	13983
Ensembl	ENSG00000140009	ENSMUSG00000021055
UniProt	Q92731	O08537
RefSeq (mRNA)	NM_001040275	NM_010157
RefSeq (protein)	NP_001035365	NP_034287
Location (UCSC)	Chr 14: 64.08 – 64.34 Mb	Chr 12: 76.12 – 76.18 Mb
PubMed search	[1]	[2]

Estrogen receptor beta (ER-β), also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2), is one of two main types of estrogen receptor, a nuclear receptor which is activated by the sex hormone estrogen. In humans, ER-β is encoded by the ESR2 gene.

Function

ER-β is a member of the family of estrogen receptors and the superfamily of nuclear receptor transcription factors. The gene product contains an N-terminal DNA binding domain and C-terminal ligand binding domain and is localized to the nucleus, cytoplasm, and mitochondria. Upon binding to 17-β-estradiol, estriol or related ligands, the encoded protein forms homo-dimers or hetero-dimers with estrogen receptor α that interact with specific DNA sequences to activate transcription. Some isoforms dominantly inhibit the activity of other estrogen receptor family members. Several alternatively spliced transcript variants of this gene have been described, but the full-length nature of some of these variants has not been fully characterized.

ER-β may have anti-proliferative effects and therefore oppose the actions of ERα in reproductive tissue. ER-β may also have an important role in adaptive function of the lung during pregnancy.

ER-β is a potent tumor suppressor and plays a crucial role in many cancer types such as prostate cancer.

Tissue distribution

ER-β is expressed by many tissues including the uterus, blood monocytes and tissue macrophages, colonic and pulmonary epithelial cells and in prostatic epithelium and in malignant counterparts of these tissues. Also, ER-β is found throughout the brain at different concentrations in different neuron clusters.

ER-β abnormalities

ER-β function is related to various cardiovascular targets including ATP-binding cassette transporter A1 (ABCA1) and apolipoprotein A1 (ApoA-1). Polymorphism may affect ER-β function and lead to altered responses in postmenopausal women receiving hormone replacement therapy.

Ligands

Agonists

Agonists of ER-β selective over ERα include:

• 3β-Androstanediol (3β-diol) – endogenous
• 8β-VE₂
• AC-186
• Apigenin – phytoestrogen
• Daidzein – phytoestrogen
• Dehydroepiandrosterone (DHEA) – endogenous
• Diarylpropionitrile (DPN)
• ERB-196 (WAY-202196)
• FERb 033 – 62-fold selectivity for ER-β over ERα
• Genistein – phytoestrogen; 16-fold selectivity for ER-β over ERα
• Kaempferol – phytoestrogen
• Liquiritigenin (Menerba) – phytoestrogen
• Penduletin – phytoestrogen
• Prinaberel (ERB-041, WAY-202041)
• S-Equol ((S)-4',7-isoflavandiol) – phytoestrogen; 13-fold selectivity for ER-β over ERα
• WAY-166818
• WAY-200070

Antagonists

Antagonists of ER-β selective over ERα include:

• PHTPP
• (R,R)-Tetrahydrochrysene ((R,R)-THC) – not actually selective over ERα, but rather an agonist instead of antagonist of ERα

Interactions

Estrogen receptor beta has been shown to interact with:

• CCND1,
• ESR1
• MAD2L1,
• NCOA3,
• NCOA6,
• RBM39, and
• SRC.

External links

• Estrogen Receptor beta at the US National Library of Medicine Medical Subject Headings (MeSH)

This article incorporates text from the United States National Library of Medicine, which is in the public domain.