ANG/PEG‐UCNPs can sequentially target the LRP on both BBB and glioma cells, leading to precise localization and enhanced accumulation at glioma site (Figure 5A).[161] As a consequence, ANG/PEG‐UCNPs functioned as a magnetic imaging/fluorescence imaging agent and showed an improved imaging performance at glioma site compared to clinically used single MRI contrast (Gd‐DTPA) and fluorescent dye (5‐ALA). This evidence concerns the gene LRP1 and central nervous system cancer.