Apitolisib is an Orally Active Class I PI3K and mTORC1/2 Inhibitor
Activation of the pathway occurs following activating point mutations or amplification of the PIK3CA gene encoding the p110a PI3K isoform. Oncogenes such as PI3K, AKT, epidermal growth factor receptor (EGFR), and human epithelial growth factor receptor 2 (HER2) stimulate proliferation, growth, and survival by activating mTOR kinase. The mTOR...
Miransertib is an Orally Active, Selective and Allosteric Akt Inhibitor
The AGC kinases AKT1, AKT2, and AKT3 are key mediators of the PI3K/AKT/mTOR signaling pathway. Additionally, AKT promotes diverse physiological processes, including cell proliferation, migration, and protein synthesis, et al. In this article, we will introduce an allosteric Akt inhibitor, Miransertib. As a potent inhibitor, Miransertib exhibits IC50s of...
COTI-2 is an Orally Available Mutant p53 Activator
TP53 (p53) is the single most frequently altered gene in human cancers, with mutations being present in approximately 50% of all invasive tumors. Besides, p53 is mutated in at least 80% of samples in some of the most difficult-to-treat cancers. Therefore, the mutant p53 protein is an important candidate...
Alobresib is an Orally Active BET Bromodomain Inhibitor for Uterine Serous Carcinoma Treatment
Uterine serous carcinoma is a rare and highly aggressive variant of endometrial cancer. Uterine serous carcinoma accounts for 10% of all endometrial cancer; however, it carries the poorest prognosis, with 5-year survival rates as low as 55%. Whole-exome sequencing studies have recently reported c-Myc gene amplification in a large...