Pep-1 was used to overcome the blood–brain tumor barrier (BBTB) and home to glioma cells via interleukin-13 receptor-α2-mediated endocytosis, and CREKA was used to bind to fibrin–fibronectin complexes abundantly expressed in tumor microenvironment for enhanced retention in the GBM. Here, FN1 is linked to central nervous system cancer.