[HTML][HTML] Design of novel and selective inhibitors of urokinase-type plasminogen activator with improved pharmacokinetic properties for use as antimetastatic agents

A Schweinitz, T Steinmetzer, IJ Banke, MJE Arlt… - Journal of Biological …, 2004 - ASBMB
The serine protease urokinase-type plasminogen activator (uPA) interacts with a specific
receptor (uPAR) on the surface of various cell types, including tumor cells, and plays a
crucial role in pericellular proteolysis. High levels of uPA and uPAR often correlate with poor
prognosis of cancer patients. Therefore, the specific inhibition of uPA with small molecule
active-site inhibitors is one strategy to decrease the invasive and metastatic activity of tumor
cells. We have developed a series of highly potent and selective uPA inhibitors with a C …