Parker Hughes Cancer Center

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Parker Hughes Institute scientists report design of new anti-cancer drug

Drug is synthetic reproduction of marine sponge

March 30, 2000, Saint Paul, Minn. ( Parker Hughes Institute researchers report potent anti-cancer activity of a novel drug. The findings of this report are published in this month¹s issue of Bioorganic & Medicinal Chemistry Letters. This drug, SPIKET-P, is a synthetic analog of spongistatin, a very powerful anti-cancer drug from a marine sponge found in the Indian Ocean. Spongistatin is a natural product that represents a unique class of anti-cancer agents. Using structure-based design and an atomic protein model, researchers prepared synthetic drugs as imitations of Spongistatin 1 as potent anti-cancer agents. At very low doses, this new agent, SPIKET-P, showed potent activity against breast, prostate, and lung cancer. It is active against taxol resistant and multi-drug resistant cancers.

Breast cancer is the most widespread cancer in women, representing 32% of all new cases and causing 18% of the cancer related deaths among women in the United States. In cancers most effecting men, a malignant prostate tumor causing prostate cancer is one of the most common cancers, representing 36% of all new cancer cases and causing 14% of the cancer related deaths in the United States. Currently, the major challenge in the treatment of breast and prostate cancer is to cure patients whose cancer has spread elsewhere in the body. Consequently, development of new potent anti-cancer drugs and the design of combination treatment protocols have emerged as areas of high priority in research.

Since the initial discovery of spongistatin in 1993, this research marks the first time that researchers prepared a synthetic analog of spongistatin. These studies provide the basis for the development of SPIKET-P as a new class of anti- cancer agents. It is anticipated that SPIKET-P and other such agents under development will be effective against other cancers, including colon cancer.

Reference: Uckun FM, Mao C, Vassilev A, Huang H, Jan S. Structure-based design of a novel synthetic spiroketal pyran as a pharmacophore of the marine natural product Spongistatin 1. Bioorganic & Medicinal Chemistry Letters, 10:541-545, 2000.

The Parker Hughes Institute, located in Roseville, Minnesota, is a non-profit research organization dedicated to combating cancer, AIDS, and diseases of the immune system.