10.26180/5c3e6c8c7e004 GUOJIE WU GUOJIE WU Structural and Functional Studies of Plasmin Inhibitors Monash University 2019 Structural Biology Fibrinolysis Protease Inhibitors Proteins and Peptides Biophysics Structural Biology (incl. Macromolecular Modelling) Biochemistry 2019-01-15 23:28:10 Thesis https://bridges.monash.edu/articles/thesis/Structural_and_Functional_Studies_of_Plasmin_Inhibitors/7591178 Human plasmin is a plasma serine protease that plays key roles in fibrinolysis, wound healing and cell migration. Accordingly, anti-fibrinolytics targeting plasmin have been widely used for treating life-threatening bleeding during surgeries or in trauma. However, current plasmin-targeting drugs are limited by poor potency or low specificity. Our researcher here characterized the functions and structures of different plasmin specific inhibitors and illustrated the inhibition mechanisms mainly via X-ray crystallography. This work revealed distinct structural features of plasmin active-site within the serine protease family, and developed highly selective plasmin inhibitors, which rationalizes structure-aided drug design and future clinical studies.