Category: Non-Small Cell Lung Cancer

CAY10404 is a Highly Selective COX-2 Inhibitor

Clooxygenase (COX) is an enzyme responsible for the formation of prostaglandins from arachidonic acid, including thromboxanes and prostaglandins. Specifically, it is a member of the animal heme peroxidase family, also known as prostaglandin G/H synthase. Besides, cyclooxygenase-2 is a candidate gene for lung injury induced by mechanical ventilation. COX-2...

DM-01 is a Powerful and Selective EZH2 Inhibitor

Enhancer of zeste homolog 2 (EZH2) is a histone methyltransferase and a catalytic component of polycomb repressive complex 2 (PRC2). EZH2 catalyzes tri-methylation of histone H3 at Lys 27 (H3K27me3) to regulate gene expression through epigenetic machinery. In addition, EZH2 also functions both as a transcriptional suppressor and a...

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...

RBN-2397 is a Selective and Orally Active NAD+ Competitive PARP7 Inhibitor

PARP is a family of proteins involved in a number of cellular processes involving mainly DNA repair and programmed cell death. The PARP family comprises 17 members. PARP1, PARP2 (inhibitor Olaparib), and PARP7 are all potential anti-cancer targets. PARP7 is a member belongs to the monoPARP family. The function...

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...

BPI-9016M is an Orally Active and Selective Dual c-Met/AXL Inhibitor

c-Met is a membrane-spanning receptor tyrosine kinase. It has a high affinity for binding to hepatocyte growth factor (HGF). As we all know, HGF/c-Met signaling often involves activation of its downstream pathways. High-level Met gene amplification, mutation or protein overexpression can lead to aberrant activation of the HGF/c-Met pathway. In...