Tivantinib is a Selective c-Met Tyrosine Kinase Inhibitor
c-Met (hepatocyte growth factor receptor, HGFR) is a type of receptor tyrosine kinase which belongs to the MET family. c-Met exsists in the surfaces of various epithelial cells. Hepatocyte growth factor (HGF) is the ligand for c-Met. HGF belongs to the soluble cytokine family and is also a member...
Reversine is a ATP-Competitive Aurora Kinase Inhibitor
Aurora kinases are serine/threonine kinases that play a prominent role in mitotic regulation. The Aurora A kinase, the “polar” kinase resides at spindle poles during mitosis. It is implicated in the control of centrosome duplication, maturation, and separation. Aurora A is important for the formation of a bipolar mitotic...
Telatinib is an Orally Active Inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit
The importance of angiogenesis in solid tumor growth is well established. Inhibition of the vascular endothelial growth factor (VEGF)/VEGF receptor (VEGFR) pathway is now an approved and generally accepted treatment of lung cancer. Interestingly, bevacizumab, a monoclonal antibody against VEGF-A, is predominantly administered in combination with chemotherapy, whereas the...
Nimbolide Induces Apoptosis through Inactivation of NF-κB
The transcription factor NF-κB is a nuclear factor that binds to the enhancer element of the immunoglobulin kappa light-chain of activated B cells. NF-κB exsists in nearly all cell types and regulates many target genes with a whole variety of functions. There are five members of the NF-κB family:...
Ulixertinib is an Orally Active and ATP-Competitive ERK1/2 Inhibitor
Effective treatment for pancreatic ductal adenocarcinoma (PDAC) is an urgent, unmet medical need. Targeting KRAS, the oncogene that is present in >95% of PDAC, is a heavily pursued strategy but remains unsuccessful in the clinic. RAF or MEK inhibitors have failed to show clinical efficacy in PDAC. A report...
WAY 316606 is an Inhibitor of the Secreted Protein sFRP-1
Human sFRP-1 is a 35 kD protein consisting of 313 amino acids. It containa 2 distinct structural domains, a netrin domain, and a cysteine-rich domain (CRD). The later domain is homologous to the Fzd receptor. sFRP-1 is thought to interact with Wnt via the CRD domain in a competitive...
Pirarubicin, an Anthracycline Antibiotics, Acts as a Topoisomerase II Inhibitor
Pirarubicin has widely application in intravesical chemotherapy for bladder cancer, but drug resistance limits its efficacy; the mechanism still needs further exploration. Bladder cancer is the most common malignancy of the urinary tract in China. 75–85% of bladder cancers are grouped as non-muscle invasive bladder tumors. Intravesical chemotherapy...