A Novel Class of Proteosome Inhibitors

Summary Harvard Medical School investigators has discovered a number of anticancer small molecules, termed ubistatins, that inhibit cell cycle machinery through interference with the ubiquitin-proteasome system. Lead ubistatins were able to arrest cyclin B proteolysis in Xenopus extract assays, and were found to prevent proteasome recognition by attaching to Lys-48-linked ubiquitinated chains. The ubistatins were discovered in a rapid miniaturized assay measuring cyclin B in Xenopus cell cycle extracts, followed by verification in a reconstituted proteasome system, and in-vivo testing in mammalian cells. Strong inhibition of ubiquitin-proteasome interaction suggests that ubistatins represent a novel class of proteasome inhibitors with promising therapeutic potential.

Applications Ubistatins may likely have broad anti-cancer applications. Clinical use may eventually address multiple myeloma, prostate cancer, non-small cell lung cancer, pancreatic cancer, ovarian cancer and breast cancer. For Further Information Please Contact the Director of Business Development Katie Gordon Email: [email protected] Telephone: (617) 432-0920

Inventor(s): King, Randall W

Type of Offer: Licensing



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