Coscinosulfate, a CDC25 phosphatase inhibitor from the sponge Coscinoderma mathewsi

Bioorg Med Chem. 2001 Nov;9(11):3049-54. doi: 10.1016/s0968-0896(01)00208-5.

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).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / isolation & purification*
  • Antineoplastic Agents / pharmacology
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Porifera / chemistry*
  • Recombinant Fusion Proteins / antagonists & inhibitors
  • Sesquiterpenes / chemistry
  • Sesquiterpenes / isolation & purification
  • Sesquiterpenes / pharmacology
  • Terpenes / chemistry
  • Terpenes / isolation & purification*
  • Terpenes / pharmacology
  • cdc25 Phosphatases / antagonists & inhibitors*

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Recombinant Fusion Proteins
  • Sesquiterpenes
  • Terpenes
  • coscinosulfate
  • cdc25 Phosphatases