Barasertib, a Pro-Drug of Barasertib-hQPA, is a Highly Selective Aurora B Inhibitor
Aurora kinases play an important role during mitosis for chromosome alignment, segregation, and cytokinesis. Selective Targeting of Aurora B kinase may be a promising therapeutic approach for the treatment of a range of malignancies. In this study, researchers explored the effect of Barasertib. In particular, Barasertib is a highly...
CC-90010 is a Reversible and Orally Active BET Inhibitor
Come straight to the point, CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors. The bromodomain and extra-terminal domain (BET) proteins, epigenetic readers, recognize and bind acetylated lysine residues. The BET protein family comprises the ubiquitously expressed...
ASP4132 is an Orally Active AMPK Activator
Adenosine monophosphate (AMP)-activated protein kinase (AMPK) is an enzyme that plays a role in cellular energy homeostasis. Specifically, it is important in largely to activate glucose and fatty acid uptake and oxidation when cellular energy is low. Besides, AMP or adenosine diphosphate (ADP) levels increase during metabolic stress such...
TNP-351, an Antifolate, is a Dihydrofolate Reductase (DHFR) Inhibitor
Antifolates are a class of antimetabolite medications that block the actions of folic acid. Antimalarial antifolates have been central for prophylaxis and treatment of malaria. The success of antifolates in the treatment of tumors also leads to the use of this class of drugs in the treatment of other...
TNO155 is an Orally Active WT SHP2 Inhibitor with Antineoplastic Activity
SHP2 is a non-receptor ubiquitous protein tyrosine phosphatase and has a relatively conserved structure and function. The SHP2 includes the PTP domain, two SH2 domains, and a C-terminal tail containing two phosphorylation sites. Binding of the N-SH2 domain with the PTP domain is able to inhibit SHP2 activity. N-SH2...
DRF-1042 is an Orally Active DNA topoisomerase I Inhibitor
Inhibitors of the enzyme topoisomerase I are cytotoxic for tumor cells because of their ability to cause DNA damage. Specifically, DNA Topoisomerase I (Top1) is one main cellular factor controlling topological homeostasis. Top1 activity can relax negative supercoils by cutting one of the DNA strands. This can create a...
Alpelisib is a Selective and Orally Active PI3Kα Inhibitor for Metastatic Breast Cancer
Phosphatidylinositol-3-kinases (PI3Ks) are a family of important lipid kinases. PI3Ks are important in controlling the signaling pathways involved in cell proliferation, motility, cell death, and cell invasion. Moreover, PI3Ks control and deliver cellular signals in the PI3K/Akt/mTOR pathway by phosphorylating phosphatidylinositol 4,5-bisphosphate (PIP2) to phosphatidylinositol 3,4,5-trisphosphate (PIP3) on the...