Approaches for targeting mitochondria in cancer therapy

The recognition of the role that mitochondria play in human health and disease is evidenced by the emergence in recent decades of a whole new field of “Mitochondrial Medicine”. Molecules located on or inside mitochondria are considered prime pharmacological targets and a wide range of efforts are underway to exploit these targets to develop targeted therapies for various diseases including cancer. However the concept of targeting, while seemingly simple in theory, has multiple subtly different practical approaches. The focus of this article is to highlight these differences in the context of a discussion on the current status of various mitochondria-targeted approaches to cancer therapy. This article is part of a Special Issue entitled: Bioenergetics of Cancer.

Research Highlights
► Mitochondria have emerged as a major target for anticancer therapy.
► Drugs may be designed for selective action on mitochondrial targets.
► Drugs may be structurally modified to increase their accumulation in the mitochondria.
► Nanocarriers may mediate increased drug accumulation in the mitochondria.