Inspired by the aberrant upregulation of DNA‐repairing RAD51, scavenger receptor B type 1 (SR‐B1), and C‐C motif chemokine ligand 5 (CCL5) in GBM patients, a reduction‐sensitive nitric oxide donor conjugate of furoxans–gemcitabine (NG) is rationally synthesized and a CCL5‐modified bioinspired lipoprotein system of C‐LNG is designed, which preferentially targets the orthotopic GBM tumors and profoundly circumvents the radiotherapy resistance. The gene discussed is RAD51; the disease is glioblastoma.