Given that LRP-1-mediated transport of An2–drug conjugates currently represents one of the most promising brain-penetrating strategies, as demonstrated in clinical studies for the treatment of recurrent malignant gliomas [46], we now highlight the potential implications of MT1-MMP as an LRP-1 functional modulator, and of cell surface MMP status on LRP-dependent An2 recognition in a glioblastoma cell model. The gene discussed is LRP1; the disease is malignant glioma.