Abstract: Urokinase plasminogen activator(uPA) and urokinase plasminogen activator receptor(uPAR) system play an important role in the process of cancer invasion, metastasis and angiogenesiss, and it is closely associated with poor prognosis of tumors. Evaluate of uPAR expression level in the tumor cell is very significant for cancer prognosis, selection and assement the therapy. Molecular targeted nuclear imaging has unique advantage in testing receptor expression, several research group labeled uPAR specially ligands with different radionuclides for imaging uPAR. The first human uPAR imaging has taken in 2015. This article reviewed the research progress of uPAR-targeted molecular nuclear imaging in recent years.