Estrogen Receptor/ERR

Tamoxifen (ICI47699) is a selective and orally effective estrogen receptor modulator (SERM). Tamoxifen has both inhibitory (e.g., mammary cells) and activating (e.g., bone, liver, and uterine cells) activity against estrogens.

Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist (IC50=9.4 nM) and an agonist of GPR30. Fulvestrant has antitumor activity, inhibiting cell proliferation and inducing apoptosis and autophagy.

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

(E Z)-4-Hydroxytamoxifen (Afimoxifene) is a novel estrogen inhibitor, commonly used in research for various estrogen-dependent conditions, including cyclic mastalgia and gynecomastia.

Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.

Cholesterol (cholesteryl alcohol) is a natural product that is the major sterol in mammals and an agonist of estrogen-related receptor α (ERRα). Cholesterol is widely found in the cell membranes of animals and is also used in the synthesis of several important hormones and bile acids.

Saikosaponin D is a novel SERCA inhibitor by inhibiting NF-κB and STAT3 signaling to protect against acetaminophen-induced hepatotoxicity.

Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant  is an orally available selective estrogen receptor degrader .

Coumestrol that existed in soybean products suppresses the proliferation of ES2 cells (IC50: 50 μM). It exhibits activities against neurological disorders, cancers and autoimmune diseases.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

Liquiritigenin (4',7-Dihydroxyflavanone), a flavonoid aglycone from licorice, is a highly selective estrogen receptor β (ERβ) agonist.

Giredestrant (GDC-9545) potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity. Giredestrant, a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist.

GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM)

Bazedoxifene acetate (WAY-TES 424) is a novel selective estrogen receptor modulator (SERM).

G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).

α-Zearalenol is one of the major metabolites of Zearalenone. α-Zearalenol has structural analogy to estrogen, thus α-Zearalenol can bind to estrogen receptors (ERs).

Delphinidin chloride, a natural plant pigment found in berries and red wine, is a precursor of certain anthocyanins. Delphinidin chloride induces the release of nitric oxide from the vascular endothelium, resulting in vascular relaxation. At the dose of 1-40 μM, epithelial growth factor receptor signaling and estrogen receptor α expression were inhibited, which was associated with apoptosis and autophagy. Delphinidin chloride regulates JAK STAT3 and MAPKinase signaling. Delphinidin also inhibited the histone acetyltransferase activity of p300 CBP (IC50 was about 30 μM).

AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity.

Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Tracheloside significantly decreases the activity of alkaline phosphatase (IC50: 0.31 μg ml), a level of inhibition comparable to that of tamoxifen (IC50: 0.43 μg ml).

Erteberel (LY500307) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.

(Rac)-Acolbifene (EM-343) is the racemic form of Acolbifene. Acolbifene is a estrogen receptor antagonist. (Rac)-Acolbifene exhibits anti-estrogenic and estrogenic activities. (Rac)-Acolbifene contains a piperidine ring and exhibits good pharmacological profile,relative binding affinity (RBA)=380.

Droloxifene (3-Hydroxytamoxifen), a tamoxifen derivative, is an oral active and selective estrogen receptor modulator.Droloxifene induced p53 expression and apoptosis in McF-7 cells.Fluroxifene has anti-estrogen and anti-implantation effects.Fluroxifene prevented bone loss in ovariectomized rats.