Ectopeptidases are widely distributed among various cell systems. Their expression on an appropriate cell type is finely regulated, reflecting the specific functional cell implications and engagement in defined physiological pathways. Protein turnover, ontogeny, inflammation, tissue remodelling, cell migration and tumor invasion are among the many physiological and pathological events in which cell-surface proteases play a crucial role, both as effector as well as regulatory molecules. It has recently become clear that also non-catalytic effects of membrane-bound proteases are of great importance in some biological regulations. They may generate specific signal transduction intracellularly, after reacting with certain target molecules. They may also play a pivotal role in cell-cell and cell-virus contact and recognition, as well as in binding to the extracellular matrix. This short review provides some insight into the multifunctional mechanisms attributed to cell membrane-bound proteases.