Plasmin (PLM), via activation from plasminogen (PLG), not only exerts fibrinolysis and thrombolysis effects, but also involves in extensive physical processes such as embryonic development, tissue remodeling and wound healing. Moreover, recent studies showed a tough association between PLM with inflammation, autoimmunity, malignancy and neural degeneration. Furthermore, more than ten plasminogen receptors and binding proteins have been discovered on cellular surface. Here, we review the researching progresses on the structures, signal transduction and pathogenic mechanisms of these receptors and binding proteins, so as to provide clues for better understanding on fibrinolysis system and for developing new diagnostic and therapeutic pathways.