Category: ER+ Breast Cancer

Capivasertib (AZD5363) is an Orally Active pan-AKT Kinase Inhibitor

Akt/PKB (Protein kinase B), usually called Akt, is a serine/threonine protein kinase with antiapoptotic activity. In addition, Akt consists of three isoforms: PKBα/Akt1, PKBβ/Akt2 and PKBγ/Akt3. Catalytically active Akt regulates the function of numerous substrates involved in cell survival, growth, proliferation, metabolism and protein synthesis. Akt possesses a protein...

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...

Telaglenastat is a Selective and Orally Active Inhibitor of Glutaminase 1

Tumor cells use a variety of oncogenically- and environmentally driven metabolic pathways. That aims to meet the bioenergetic and biosynthetic demands of rapid and sustained growth. One of the key nutrients is the amino acid glutamine. It is the most abundant amino acid in plasma. Small-molecule inhibitors, suppressing the...

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,...