Enzyme-mediated dual-targeted-assembly realizes a synergistic anticancer effect.

We designed and synthesized homochiral-peptide-based boron diketonate complexes. Co-administration of the two stereoisomers in cancer cells led to molecular assembly targeting both the plasma membrane and the lysosomes mediated via membrane-bonded enzymes. The dual-targeted-assembly generates a synergistic anticancer effect with amplified cancer spheroid toxicity and enhanced inhibition efficacy on cancer cell migration.