Tag: Estrogen Receptor

ARV-471 is an Estrogen Receptor PROTAC Degrader for Breast Cancer

PROTAC is a heterobifunctional molecule containing two small molecule binding moieties. Specifically, PROTACs in cells seek and selectively bind to target proteins. PROTAC then recruits specific E3 ligases to the target protein. Besides, it forms a ternary complex in close proximity to the target protein and E3 ligase. In...

GNE-149 is an Orally Active Estrogen Receptor α Antagonist

Estrogen receptor α (ERα) and β (ERβ) is a nuclear transcription factors involved in regulating many complex human physiological processes. Moreover, these proteins play a role in the nucleus and regulate the transcription of specific target genes by binding with relevant DNA regulatory sequences. The interaction between ligands, receptors,...

MS4322 is a First-in-Class PRMT5 PROTAC Degrader

PRMT5 is a member of type II protein arginine methyltransferases (PRMTs). When interacting with its binding partner MEP50, PRMT5 catalyzes monomethylation and symmetric dimethylation of arginine residues of its histone substrates. These substrates include H3R2, H3R8, and H4R3, and its nonhistone substrates, including p53, EGFR, N-MYC, SmD3, and RNA...

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,...

H3B-6545 is an Orally Active and Selective ER Covalent Antagonist (SERCA)

Breast cancer is the second leading cause of cancer mortality among women worldwide. Estrogen receptor alpha (ERα) is a key hormone-regulated transcription factor for normal and malignant breast cells. Moreover, tumors that are ER-positive are much more likely to respond to treatments that block estrogen in ER-positive/HER2 negative breast...

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...