Tag: Estrogen Receptor

Breast cancer is subdivided into categories based on the tumor receptor status. Specifically, whether the tumor expresses estrogen receptor (ER), progesterone receptor (PR), or Her2. And, with ER+ disease makes up the majority of patients in the breast cancer patient population. Although there are currently available drugs against ER-positive...

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...

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,...

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...

The estrogen receptor (ER) is expressed in the majority of breast tumors and in a number of endocrine tissues including the normal breast, uterus, and vagina, as well as in the pituitary and hypothalamus. Fulvestrant is the first of a new type of endocrine treatment——an oestrogen receptor (ER) 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,...

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...