title: Coscinosulfate, a CDC25 phosphatase inhibitor from the sponge Coscinoderma mathewsi.
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).
authors.affiliation: Laboratoire de Chimie des Substances Naturelles, Muséum d'Histoire Naturelle, associé au CNRS, Paris, France.
authors.forename: A
authors.initials: A
authors.lastname: Loukaci
authors.forename: I
authors.initials: I
authors.lastname: Le Saout
authors.forename: M
authors.initials: M
authors.lastname: Samadi
authors.forename: S
authors.initials: S
authors.lastname: Leclerc
authors.forename: E
authors.initials: E
authors.lastname: Damiens
authors.forename: L
authors.initials: L
authors.lastname: Meijer
authors.forename: C
authors.initials: C
authors.lastname: Debitus
authors.forename: M
authors.initials: M
authors.lastname: Guyot
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D011161:Porifera / Q000737:chemistry*; D011993:Recombinant Fusion Proteins / Q000037:antagonists & inhibitors; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D013729:Terpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D020687:cdc25 Phosphatases / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011993:Recombinant Fusion Proteins; D012717:Sesquiterpenes; D013729:Terpenes; C449079:coscinosulfate; D020687:cdc25 Phosphatases