The role of urokinase in matrix invasion and degradation by a variety of tumour cells, as well as in other invasive processes associated with both normal and pathological states has been well documented in recent years. Active site inhibitors of urokinase would provide a tool to assess the function of the enzyme in these processes. If urokinase proves to be a critical element, some of these inhibitors may also serve as lead compounds for potential therapeutic agents. Nevertheless, reports on small, synthetic, and competitive inhibitors of urokinase have been relatively few compared to inhibitors of other proteases. This paper reviews published work on competitive inhibitors of urokinase.
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