With the aim of exploiting the upregulation of LRP1 receptor in both BBB and GBM cells, a novel targeting stapled peptide was synthesized and conjugated onto PEGylated polylactic acid polymeric micelles by Ruan et al. The peptide ST-RAP12, derived from the RAP protein, had a higher LRP1-binding affinity and uptake in endothelial and GBM cells than the non-stapled form. The gene discussed is LRPAP1; the disease is glioblastoma.