ABSTRACT

As the cell’s power plants, the mitochondria provide the cell with ATP through oxidative phosphorylation. However, they are also key players in biosynthesis and regulated cell death. It is therefore not surprising that they have emerged as promising drug targets in cancer chemotherapy. Mitochondria-targeting drugs can bypass resistance mechanisms and (re-)activate cell death programs in tumor cells. The mitochondria 68are ideal targets of metallo-drugs, as many metal complexes tend to accumulate in the mitochondria because of their lipophilicity and positive charge or can be conveniently functionalized with mitochondria-directing entities. This chapter starts with an overview on the role of the mitochondria in cell death, disease, and cancer. We then discuss recent developments of mitochondria-targeting platinum, gold, ruthenium, iridium, rhenium, and copper complexes as well as metal-based photosensitizers.