For these perspectives, we herein synthesized a reduction‐sensitive NO donor conjugate of furoxans–gemcitabine (Gem, a RAD51 inhibitor) (NG) as radio‐sensitizer and then rationally designed a CCL5 peptide‐modified bioinspired lipoprotein system of NG (C‐LNG), aiming to preferentially target the GBM tumor sites and potentiate the RT efficacy (Figure 1H). The gene discussed is RAD51; the disease is glioblastoma.