1. Coscinosulfate, a CDC25 phosphatase inhibitor from the sponge Coscinoderma mathewsi.
- Author
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Loukaci A, Le Saout I, Samadi M, Leclerc S, Damiens E, Meijer L, Debitus C, and Guyot M
- Subjects
- Animals, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Enzyme Inhibitors chemistry, Enzyme Inhibitors isolation & purification, Enzyme Inhibitors pharmacology, Humans, Inhibitory Concentration 50, Magnetic Resonance Spectroscopy, Molecular Structure, Recombinant Fusion Proteins antagonists & inhibitors, Sesquiterpenes chemistry, Sesquiterpenes isolation & purification, Sesquiterpenes pharmacology, Terpenes chemistry, Terpenes pharmacology, Antineoplastic Agents isolation & purification, Porifera chemistry, Terpenes isolation & purification, cdc25 Phosphatases antagonists & inhibitors
- 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).
- Published
- 2001
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