Estrogen and Related Receptors

Estrogen controls many cellular processes including growth, differentiation and function of the reproductive system. Estrogen is also responsible for the growth and maintenance of the skeleton and the normal function of the cardiovascular and nervous systems.

Products
Background
Literature
Pathways
Gene Data

Agonists

Cat No Product Name / Activity
5053 AC 186
Potent and selective ERβ agonist; neuroprotective
1417 Daidzein
Estrogen receptor agonist. Also induces cell cycle arrest
1494 DPN
Highly potent ERβ agonist
4494 (R)-DPN
Enantiomer of DPN (Cat. No. 1494)
2266 DY131
Agonist selective for estrogen-related receptors ERRβ and ERRγ
6158 (S)-Equol
Potent estrogen receptor β (ERβ) agonist; dihydrotestosterone antagonist
4276 ERB 041
Potent ERβ agonist
2823 α-Estradiol
Endogenous estrogen receptor agonist
2824 β-Estradiol
Endogenous ER agonist
3588 Estropipate
Estrogen receptor agonist and OATP1B1 inhibitor
3523 FERb 033
Potent and selective ERβ agonist
3075 GSK 4716
Selective ERRγ and ERRβ agonist
3907 27-Hydroxycholesterol
ER partial agonist; also LXR agonist
3819 Liquiritigenin
Selective ERβ agonist
1426 PPT
Subtype-selective ERα agonist
3366 WAY 200070
Selective ERβ agonist

Antagonists

Cat No Product Name / Activity
1047 ICI 182,780
Estrogen receptor antagonist
1991 MPP dihydrochloride
Highly selective ERα antagonist
2662 PHTPP
Selective ERβ antagonist
3928 XCT 790
Selective ERRα antagonist/inverse agonist
2183 ZK 164015
Potent estrogen receptor antagonist

Modulators

Cat No Product Name / Activity
5263 Bazedoxifene acetate
Potent and selective estrogen receptor modulator (SERM)
5421 BTC
Selective estrogen receptor modulator (SERM)
3999 Cyclofenil
Selective estrogen receptor modulator (SERM)
3412 (Z)-4-Hydroxytamoxifen
Metabolite of tamoxifen (Cat. No. 0999)
2280 Raloxifene hydrochloride
Selective estrogen receptor modulator (SERM)
0999 Tamoxifen citrate
Estrogen receptor partial agonist/antagonist
2676 Y 134
Selective estrogen receptor modulator (SERM), selective for ERα

Inhibitors

Cat No Product Name / Activity
4382 Letrozole
Potent, reversible non-steroidal aromatase inhibitor

Other

Cat No Product Name / Activity
3388 Anastrozole
Potent aromatase (CYP19) inhibitor
0743 DPPE fumarate
Ligand for anti-estrogen binding site
3705 Endoxifen
Potent antiestrogen; ERα ligand
1110 Genistein
Estrogen receptor ligand. Also tyrosine kinase inhibitor
3224 RU 58668
Pure antiestrogen
1990 (R,R)-THC
Potent subtype-selective ligand; ERα agonist/ERβ antagonist
3278 YM 511
Potent aromatase (CYP19) inhibitor
3975 Zearalenone
Estrogen receptor ligand; mycotoxin

Estrogen controls many cellular processes including growth, differentiation and function of the reproductive system. In females, estrogen's main targets are the ovaries, uterus, vagina and mammary glands. In the male, target organs are the testes, prostate and epididymis. Estrogen is also responsible for the growth and maintenance of the skeleton and the normal functioning of the cardiovascular and nervous systems.

Estrogen exerts most of its actions via estrogen receptors (ER). Estrogen receptors are ligand-activated transcription factors belonging to the nuclear hormone receptor superfamily.

Today, two estrogen receptors are known, ERα and ERβ. ERα protein is highly homologous to ERβ protein, especially in the DNA and ligand binding domains, although divergence exists in the N-terminal transactivation domain. Both receptors interact with the same DNA response element and show a similar ligand binding profile. Upon ligand binding estrogen receptors undergo a conformational change allowing spontaneous dimerization to form either homo- or heterodimers. As a dimer, the estrogen receptor binds to the estrogen response element (ERE) in the promoter region of target genes. ERα and ERβ are present in a broad spectrum of tissues.

Three estrogen-related receptors (ERRs) - ERRα, ERRβ and ERRγ - have also been identified. Classified as 'orphan' nuclear receptors, they do not bind endogenous estrogens; instead, they are activated by co-regulatory proteins and bind the ERE and ERR response elements (ERREs) as homodimers, exerting transcriptional control of energy homeostasis. As a result, they may be useful therapeutic targets for metabolic diseases, such as obesity and diabetes, as well as cancer.

External sources of pharmacological information for Estrogen and Related Receptors :

    Literature for Estrogen and Related Receptors

    Cancer

    Cancer Research Product Guide

    A collection of over 750 products for cancer research, the guide includes research tools for the study of:

    • Cancer Metabolism
    • Epigenetics in Cancer
    • Receptor Signaling
    • Cell Cycle and DNA Damage Repair
    • Angiogenesis
    • Invasion and Metastasis
    Nuclear Receptors

    Nuclear Receptors Product Listing

    A collection of over 150 products for key nuclear receptors, the listing includes research tools for the study of:

    • Androgen Receptors
    • Estrogen Receptors
    • Retinoic Acid Receptors
    • Retinoid X Receptors
    • Vitamin D Receptors

    Pathways for Estrogen and Related Receptors

    Estrogen

    Estrogen Signaling Pathway

    Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.

    Estrogen Receptor Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    ERα Human ESR1 NM_001122742 P03372
    Mouse Esr1 NM_007956 P19785
    Rat Esr1 NM_012689 P06211
    ERβ Human ESR2 NM_001040275 Q92731
    Mouse Esr2 NM_207707 O08537
    Rat Esr2 NM_012754 Q62986
    ESRRα Human ESRRA NM_004451 X51416
    Mouse Esrra NM_007953 O08580
    Rat Esrra NM_001008511 Q5QJV7
    ESRRβ Human ESRRB NM_004452 X51417
    Mouse Esrrb NM_011934 Q61539
    Rat Esrrb NM_001008516 P11475
    ESRRγ Human ESRRG NM_206595 AF058291
    Mouse Esrrg NM_011935 P62509
    Rat Esrrg NM_203336 P62510