JX06 is a Potent, Selective and Covalent Inhibitor of PDK
Pyruvate dehydrogenase kinase (PDK) is a kinase that can be inactivated by the use of ATP phosphorylation of pyruvate dehydrogenase. Specifically, PDK is relevant to the regulation of the pyruvate dehydrogenase complex with pyruvate dehydrogenase as the first component. Besides, PDK acts as a molecular switch to reduce mitochondrial...
ONO-7475 is a Selective and Orally Active AXL/Mer Inhibitor
EGFR tyrosine kinase inhibitors (EGFR-TKIs) are efficient for the treatment of non-small cell lung cancer (NSCLC) harboring EGFR mutations. However, most EGFR-positive NSCLC patients exhibit resistance to EGFR-TKIs after sometimes. The 3rd generation EGFR-TKI Osimertinib shows efficacy for overcoming EGFR T790M mutation-positive NSCLC. Anexelekto (AXL) belongs to the TAM...
TP3011 is a Potent Topoisomerase-1 Inhibitor with Anti-tumor Effect
Topoisomerases are proteins that cut the DNA backbone. Especially, topoisomerases let the cut ends twist past each other to a more relaxed configuration. Moreover, topoisomerases reseal the phosphodiester bonds in the backbone to again form an intact double helix. DNA topoisomerases I and II present in cells acts through...
AMG-510 is a First-in-Class, Orally Active, and Selective KRAS G12C Inhibitor
The KRAS oncoprotein is a GTPase and an essential mediator of intracellular signaling pathways. They are involved in tumor cell growth and survival. Somatic, activating mutations in KRAS are a hallmark of cancer. Furthermore, they prevent the association of GTPase-activating proteins, thus stabilizing effector binding and enhancing KRAS signaling....