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Coscinosulfate, a CDC25 phosphatase inhibitor from the sponge Coscinoderma mathewsi
A Loukaci1, I Le Saout, M Samadi
1Laboratoire de Chimie des Substances Naturelles, Muséum d'Histoire Naturelle, associé au CNRS, Paris, France.
Bioorganic & Medicinal Chemistry
|October 13, 2001
Abstract:
The dual specificity CDC25 phosphatases dephosphorylate two inhibitory phospho-amino acids of cyclin-dependent kinases, a major family of cell cycle regulators. CDC25 inhibitors constitute new anti-mitotic agents with potential anticancer activity. While screening through a collection of natural products derived from marine organisms for CDC25A inhibitors, we purified and identified coscinosulfate 1, a sesquiterpene sulfate from the New Caledonian sponge Coscinoderma matthewsi, along with 4. The purified compound 1 displayed significant inhibitory activity towards CDC25A (IC(50): 3 microM).