The Asn–Gly–Arg (NGR) motif that facilitates the uptake of micelles by CD13-overexpressed tumor cells (fibrosarcoma, HT1080) and HUVEC in BALB/c mice bearing HT1080 tumor xenografts showed a stronger efficacy and less body weight changes in the NGR–PM-DTX group. Here, ANPEP is linked to neoplasm.