A novel mitochondriotoxic small molecule that selectively inhibits tumor cell growth.

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.

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@article{Fantin2002ANM, title={A novel mitochondriotoxic small molecule that selectively inhibits tumor cell growth.}, author={Valeria R. Fantin and Marcelo J. Berardi and Luca Scorrano and Stanley J . Korsmeyer and Philip Leder}, journal={Cancer cell}, year={2002}, volume={2 1}, pages={29-42} }