F16 attacks cancer cells

In July Cancer Cell, Valeria Fantin and colleagues from Harvard Medical School, Boston, describe a novel mitochondriotoxic small molecule that selectively inhibits tumor cell growth (Cancer Cell 2002, 2:29-42).

Fantin et al. used a cell-based assay to perform a high-throughput chemical library screen and identified F16, a small molecule that belongs to a group of structurally similar compounds with a delocalized positive charge. They observed that F16 selectively inhibits proliferation of mammary epithelial, neu-overexpressing cells, as well as a variety of mouse mammary tumor and human breast cancer cell lines.

In addition, they show that F16 is accumulated in the mitochondria of responsive cells, driven by the membrane potential, and that it compromises mitochondrial functional integrity.

"Therapeutic interventions that can selectively target the mitochondria of transformed cells and trigger the apoptotic cascade without relying on intact upstream apoptosis-inducing pathways could represent a specific, low...