Abstract
We hereby engineered photoactivatable Pt(
iv
) metallodrugs that harness CD36 to target ovarian cancer cells. Pt(
iv
) compounds mimic the structure of fatty acids and take advantage of CD36 as a “Trojan horse” to gain entry into the cells. We confirmed that CD36-dependent entry occurs using graphite furnace atomic absorption spectroscopy with ovarian cancer cells expressing different levels of CD36 and a CD36 inhibitor, SSO. Once the Pt(
iv
) metallodrugs enter the cancer cells, they can be activated to form Pt(
ii
) with characteristics of cisplatin under visible light (490 nm) irradiation, promoting photoinduced electron transfer from the attached fluorophore to the metal center. This light-induced activation can increase the cytotoxicity of the Pt(
iv
) metallodrugs by up to 20 times toward ovarian cancer cells, inducing DNA damage and enabling efficient elimination of drug-resistant cancer cells.