SCARB1 and neoplasm: Inspired by the aberrant upregulation of RAD51 (a critical protein of DNA repair), scavenger receptor B type 1 (SR‐B1), and C‐C motif chemokine ligand 5 (CCL5) in GBM patients, a reduction‐sensitive nitric oxide (NO) donor conjugate of gemcitabine (RAD51 inhibitor) (NG) is synthesized as radio‐sensitizer and a CCL5 peptide‐modified bioinspired lipoprotein system of NG (C‐LNG) is rationally designed, aiming to preferentially target the tumor sites and overcome the RT resistance.