Abstract: The urokinase-type plasminogen activator receptor (uPAR) is a glysocylphosphatidylinositol (GPI) anchor protein, which regulates proteolysis and cooperate with transmembrane receptors to activate a series of signaling pathways in cells, promoting cell proliferation, invasion and migration. Meanwhile, uPAR was overexpressed in a panel of malignancies, which has become a potential target for tumor diagnosis and treatment. At present, imaging techniques for tumor diagnosis mainly include X-ray, computed tomography, nuclear magnetic resonance and positron emission tomography(PET), among which PET has received extensive attention due to its ultra-high sensitivity and specificity. Accumulating reports have shown that PET imaging with small molecules and antibody targeting uPAR could achieve localization and quantitative detection of tumor cells. At the same time, the proliferation, invasion and migration of colon cancer, breast cancer and ovarian cancer could be significantly inhibited by blocking the interaction between uPA and uPAR or repressing the expression of uPAR in cancer therapy. In this review, we summarized the role of PET imaging with small molecules and antibody targeting uPAR for tumor diagnosis and the research progress of uPAR for tumor-targeted therapy. 

Key words: font-size:medium, ">uPAR； PET imaging； diagnosis； tumor therapy