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...
IACS-15414 is an Orally Active SHP2 Inhibitor
Src-homology-2-containing protein tyrosine phosphatase 2 (SHP2), encoded by the PTPN11 gene, is a classical nonreceptor protein tyrosine phosphatase (PTP). SHP2 is a ubiquitous protein tyrosine phosphatase with a relatively conserved structure and function. It has emerged as a key downstream regulator of several receptor tyrosine kinases (RTKs) and cytokine...
β-Lapachone, a Naturally Occurring O-naphthoquinone, is a Topoisomerase I Inhibitor
β-Lapachone is an ortho-naphthoquinone and inhibits topoisomerase I. β-Lapachone is a classic quinone-containing antitumor NQO1-bioactivatable drug that directly kills NQO1-overexpressing cancer cells. NQO1 is an antioxidative enzyme that helps recover renal oxidative status. β-Lapachone reduces cisplatin-induced nephrotoxicity. In cancer cells, cisplatin forms cross-link with DNA, which inhibits DNA replication,...