Abstract
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Breast cancer is the most common malignancy afflicting Western
women today and causes many deaths due to metastatic disease. Upregulation of
the plasminogen-activation system (PAS) strongly correlates with poor prognosis
in metastatic breast cancer and targeting this system is a promising strategy for
developing prophylactic anti-metastasis drugs. Two classes of PAS-targeting
agents are inhibitors of the serine protease activity of urokinase plasminogen
activator (uPA) and antagonists of the interaction of uPA with its cell surface
receptor (uPAR). This review provides an overview of the role of PAS in cancer
metastasis before discussing the small molecules and peptides from the patent
literature since 2000 that target either uPA or uPA/uPAR interactions for use as
anti-metastasis drugs