Elacestrant (RAD1901) is an Orally Available Estrogen Receptor Degrader
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...
CYD-4-61 is a Bax Activator Used for Breast Cancer Research
Bax is an apoptosis regulator, belonging to the Bcl-2-like protein family. It controls mitochondrial dysfunction and apoptosis. Bax can promote apoptosis by forming a heterodimer with Bcl-2 to become a lethal mitochondrial pore protein. Specifically, it can induce mitochondrial outer membrane permeability, release cytochrome c, and cause programmed death...
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...
Vistusertib (AZD2014) is an ATP Competitive mTOR Inhibitor
mTOR is an atypical serine threonine kinase involved in regulating major cellular functions, such as nutrients sensing, growth, and proliferation. mTOR is part of the multiprotein complexes mTORC1 and mTORC2. mTORC1 and mTORC2 have been shown to play critical yet functionally distinct roles in the regulation of cellular processes....
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...
SAR439859 is an Orally Active, Nonsteroidal and Selective Estrogen Receptor Degrader
It is estimated that worldwide 6270001 women died in 2018 due to breast cancer. Breast cancer is the most common cancer in females. In addition, Breast cancer (BCs) can be classified into three groups. BC includes Estrogen Receptor positive (ER+) and/or Progesterone Receptor positive (PR+) (represent about 75% of...