Tag: ER

Acolbifene (EM-652), is an Orally Active Selective Estrogen Receptor Antagonist

There are two different forms of the estrogen receptor ERα and ERβ. Acolbifene (EM-652) is an orally active selective estrogen receptor antagonist. In particular, Acolbifene is a cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene exerts a potent and pure anti-estrogenic action in the mammary gland and uterus. In addition,...

Elacestrant is an Orally Available SERD (Estrogen Receptor Degrader )

Estrogen receptor (ER) is a ligand-induced intracellular transcription factor that mediates the biological effects of estrogen at the level of most gene regulation. The biological effect of estrogen is mediated by ER, which is a member of nuclear receptor family. Specifically, these receptors act as ligand-activated transcription factors. There...

FLTX1, a Fluorescent Tamoxifen Derivative, Specifically Labels Intracellular Binding Sites (ER)

Tamoxifen is a nonsteroidal agent and competitively binds to estrogen receptors (ER). This compound itself is a prodrug and it has a relatively little affinity for ER. However, tamoxifen can transform into active metabolites 4-hydroxytamoxifen and N-desmethyl-4-hydroxytamoxifen (endoxifen). Besides, these metabolites exhibit 30–100 times more affinity with the estrogen...

Giredestrant is an Orally Active and Selective ER Antagonist

Estrogen receptor (ERs) is a group of proteins found in cells and is activated by estrogen. Specifically, ERs are typical members of the nuclear receptor superfamily, including receptors that mediate steroid hormones, thyroid hormones, vitamin A and vitamin D, and many orphan receptors. Besides, once ER is activated, estrogen...

AZD-9833 is an Orally Active Estrogen Receptor (ER) Antagonist

Estrogens participate in numerous physiological processes such as cell growth, reproduction, and differentiation. In females, the ovaries are the major site of estrogen synthesis producing the predominant estrogen 17b-estradiol (E2). In addition to effects by E2 on normal physiology, estrogens also play an important role in several pathological processes...

UT-34 is an Orally Active pan-Androgen Receptor Degrader (SARD)

Prostate cancer drugs targeting the androgen receptor (AR) are mainly competitive ligand-binding domain (LBD) binding antagonists. A common mechanism of drug resistance can inactivate it. Specifically, AR is a nuclear receptor that is activated by binding to any androgen. In addition, radical prostatectomy combined with gonadotropin and androgen synthetase...

ERD-308, a PROTAC Degrader of ER, Has Potential to Treat ER+ Breast Cancer Treatment

In previous blogs, I have introduced some compounds based on PROTAC technology, including SJFδ, MS4077, BSJ-03-123, A1874, HJB97, Olutasidenib. Today, I’d like to introduce another novel compound ERD-308 as a highly potent PROTAC degrader of estrogen receptor (ER). Breast cancer (BC) is a common malignancy in women worldwide. Besides,...