Synthetic urokinase inhibitors as potential antitumor drugs.

Urokinase-mediated plasminogen activation is involved in many normal physiological processes, including tissue remodeling, embryogenesis, wound healing and clot lysis. In addition, elevated levels of urokinase, the urokinase receptor uPA-R and its endogenous inhibitor plasminogen activator inhibitor (PAI-1), in combination with plasmin, play an important role in the pathogenesis of malignancy through its ability to mediate tumor cell growth, invasion and metastatic dissemination. The inhibition of urokinase with synthetic inhibitors is a new concept for a specific cancer therapy. This review examines synthetic urokinase inhibitors described during the last two years.