A novel mitochondriotoxic small molecule that selectively inhibits tumor cell growth - PubMed

A novel mitochondriotoxic small molecule that selectively inhibits tumor cell growth

Valeria R Fantin et al. Cancer Cell. 2002 Jul.

Free article

Abstract

Tumorigenesis results from events that impinge on a variety of collaborating metabolic pathways. To assess their role in this process, we utilized a cell-based assay to perform a high-throughput, chemical library screen. In so doing, we identified F16, a small molecule that selectively inhibits proliferation of mammary epithelial, neu-overexpressing cells, as well as a variety of mouse mammary tumor and human breast cancer cell lines. F16 belongs to a group of structurally similar molecules with a delocalized positive charge. The compound is accumulated in mitochondria of responsive cells, driven by the membrane potential, and it compromises their functional integrity. Mitochondrial hyperpolarization is a shared feature of many tumor cell lines, explaining the broad action spectrum of this novel delocalized lipophilic cation.

Comment in

• A mitochondrial Achilles' heel in cancer?

  Hockenbery DM. Hockenbery DM. Cancer Cell. 2002 Jul;2(1):1-2. doi: 10.1016/s1535-6108(02)00087-9. Cancer Cell. 2002. PMID: 12150816

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