Tag: ERα

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,...

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...