Journal
CELL DEATH & DISEASE
Volume 5, Issue -, Pages -Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/cddis.2014.420
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Funding
- National Cancer Institute of the National Institutes of Health [P30CA016042]
- Jonsson Cancer Center Foundation seed grant
- V Foundation for Cancer Research V Scholar Award
- University of California Cancer Research Coordinating Committee Funds
- National Science Foundation [NSF-MCB1243645]
- V Foundation-Gil Nickel Family Endowed Fellowship in Melanoma Research
- Spanish Society of Medical Oncology (SEOM) for Translational Research in Reference Centers
- NIH [K25CA157940, R01CA185189, R01CA90571, R01CA156674, R01GM073981, P01GM081621, P01CA168585]
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Cancer cell proliferation relies on the ability of cancer cells to grow, transition through the cell cycle, and divide. To identify novel chemical probes for dissecting the mechanisms governing cell cycle progression and cell division, and for developing new anticancer therapeutics, we developed and performed a novel cancer cell-based high-throughput chemical screen for cell cycle modulators. This approach identified novel G1, S, G2, and M-phase specific inhibitors with drug-like properties and diverse chemotypes likely targeting a broad array of processes. We further characterized the M-phase inhibitors and highlight the most potent M-phase inhibitor MI-181, which targets tubulin, inhibits tubulin polymerization, activates the spindle assembly checkpoint, arrests cells in mitosis, and triggers a fast apoptotic cell death. Importantly, MI-181 has broad anti-cancer activity, especially against BRAF(V600E) melanomas.
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