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.