A novel tumor and mitochondria dual-targeted photosensitizer showing ultra-efficient photodynamic anticancer activities.

We designed and synthesized a simple, but highly effective photosensitizer (G-Mito-Pc), which can precisely target the mitochondria of epidermal growth factor receptor (EGFR)-overexpressing cancer cells, to achieve dual targeting function at both cell and organelle levels in cancer therapy. We further explored the possible molecular mechanism of the enhanced bioactivity of G-Mito-Pc compared to that of the reference photosensitizer using molecular dynamics simulations on their interactions with a physiologically relevant mitochondrial membrane model.