Targefrin is a Potent EphA2 Antagonist with Antitumor Activity
EphA2, a transmembrane glycoprotein, is a type of Ephrin receptors (Eph) which is the most important class of receptor tyrosine kinases. EphA2 can be detected in most epithelial cells. In common situation, it interacts with ephrin A1 on the neighboring cell, thereby inducing diverse signaling networks following cell-to-cell contact. Ephrin...
Reversin 121, a P-glycoprotein Inhibitor, Reverses P-glycoprotein-Mediated Multidrug Resistance
Nowadays, how to overcome the resistance of tumor cells to multiple drugs is still a serious problem. Various mechanisms can cause Multidrug resistance (MDR), including cell cycle alterations, increased repair of damaged DNA and activation of detoxifying systems. Noticeably, ATP-binding cassette proteins are the most significant factor in drug...
G12Si-5 is a K-Ras G12S Mutant Covalent Inhibitor
KRAS (Kirsten rat sarcoma virus) is one of the most commonly altered oncogenes in human cancers. Recurrent oncogenic mutations in KRAS can reprogram glutamine metabolism to increase the production of NADPH to control ROS. Besides, mutant KRAS promotes the expression of nucleotide synthesis genes and controls glucose uptake and...
Certepetide is a Tumor-penetrating Enhancer via RGD Motif Interaction with Alphav-integrins
αV integrin is a protein that is encoded by the ITGAV gene. Studies show the participation of αV integrins in the proliferation, motility and proteolysis of various cancer cells. Neuropilin-1 is a membrane-bound coreceptor to a tyrosine kinase receptor for both vascular endothelial growth factor and semaphorin family members....
Panobinostat is a Potent and Orally Active Non-selective HDAC Inhibitor
HDACs (Histone deacetylases) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone, allowing the histones to wrap the DNA more tightly. This is important because acetylation and de-acetylation can regulate DNA expression. Acetylation is controlled by two antagonistic enzyme families:...
FH535 is a Potent Inhibitor of Wnt/β-catenin and PPAR
The Wnt signaling pathway is important in normal development and in cancer. This signaling pathway is regulated by Wnt ligands, the APC-Axin complex and β-catenin. Wnt/β-catenin signaling pathway plays a central role in regulating the balance between stem cell growth and differentiation. Thus, the degree of Wnt signaling activation...
PX-12 is an Irreversible Inhibitor of Thioredoxin-1 (Trx-1)
Colorectal cancer is one of the leading causes of cancer-related mortality in most industrialized nations. It needs to find an effective adjuvant therapy for colorectal cancer. There includes non-steroidal anti-inflammatory drugs, immunotherapy, and gene therapy. Thioredoxin (Trx) and thioredoxin reductase 1 are among the major redox regulators in mammalian...