The involvement of proteases in the metastatic spread of tumour cells and in tumour related processes, such as angiogenesis and ulceration, has been known for many decades. This chapter reviews the involvement of one proteolytic system--the plasminogen activation system--in tumour progression. In recent years, many biochemical properties of the various components of the plasminogen activation system have become known. These properties and the functional relationship between the components are discussed in the first section. Since interfering with proteolysis by tumour cells and by newly formed endothelial cells can be an objective for future therapy, experimental tumour models have been used to study the effects of inhibitors of plasminogen activation. The second section deals with this issue. Finally, the presence of the various components of the plasminogen activation system in human tumours is reviewed. Following the availability of specific ELISAs, antibodies and molecular probes, the content and the cellular distribution of the components of the plasminogen activation system have recently been mapped in various human tumours.