Regarding the critical role of DNA repair in RT resistance and aberrantly upregulated SR‐B1 and CCL5 in GBM tumors, we successfully synthesized a reduction‐sensitive NO donor conjugate of furoxans–gemcitabine (NG) as radio‐sensitizer and fabricated a CCL5 peptide‐modified bioinspired lipoprotein system of C‐LNG, thereby preferentially targeting the GBM tumor sites to overcome the RT resistance. The gene discussed is SCARB1; the disease is glioblastoma.