Colorectal Cancer (bowel cancer; colon cancer) is one of the most serious cancer diseases, with the development from colon or rectum. It is mainly due to old age and environmental…
TAS4464, a highly potent and selective inhibitor of NEDD8 activating enzyme, shows antitumor activity. NEDD8 activating enzyme (NAE) is an essential regulator of the NEDD8 conjugation pathway. The ubiquitin-like modifier…
In previous blog, we introduced AMG 487 as a potent, orally active and selective CXCR3 antagonist, which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50 values of…
Drugs that inhibit estrogen receptor alpha (ERα) or which block the production of estrogens remain frontline interventions in the treatment and management of breast cancer at all stages. In this…
In previous blog, we described NG25 as a potent dual TAK1 and MAP4K2 inhibitor. The compound shows excellent inhibition for inhibiting IKKβ activation by TLR7 and TLR9 agonists. Today, I’d…
De novo pyrimidine nucleotide biosynthesis is activated in proliferating cancer cells in response to an increased demand for synthesis of DNA, RNA and phospholipids. The synthesis activates via oncogenic pathways,…
Overexpression and activation of the murine double minute 2 (MDM2) or nuclear factor of activated T cells 1 (NFAT1) oncoproteins occur frequently in pancreatic cancer. Many MDM2 inhibitors target MDM2-p53…
As we all know, Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor. Aurora kinases are essential mediators in cell mitosis. Amplification of these kinases can lead to…
HDAC (Histone deacetylases) are a group of proteins that act on histones. They remove acetyl groups from N-acetyl lysine amino acid on a histone. As a result, histones wrap DNA…
The tumor suppressor p53 is a powerful growth-suppressive and proapoptotic protein. Murine double minute (MDM) 2 and MDMX, as its negative regulators, tightly controlls p53. These proteins bind p53 with…