Specific Targeting of Cell Division (and Cancer): Small molecule inhibitors of Eg5 Hold Potential for Enhanced Safety

Summary Prof. Mitchison’s group at Harvard was the first to show, very elegantly, that it is possible to specifically target cell division proteins other than tubulin by using a small molecule, monastrol, which targets Eg5 and leads to mitotic arrest. Eg5 is responsible for establishing and maintaining the bipolar spindle. This work on monastrol subsequently led to considerable activity in several fields such as in chemistry for the improved synthesis of monastrol, enantioseparation, and synthesis of monastrol analogues; in biochemistry for the in-depth characterization of the monastrol-Eg5 interaction; in structural biology for the crystallographic structure of human Eg5 in the native form and complexed with monastrol; and in cell biology for the detailed characterization of the inhibition of Eg5 during the cell cycle. The efforts at Harvard led to the identification of several compound families as Eg5 inhibitors. Some of those are being developed as anti-cancer drugs by Harvard’s partners under non-exclusive licenses. Other, identified more recently, are available for exclusive licensing.

Applications Eg5 inhibitors may be developed as anti-cancer drugs targeting a broad range of cancer types. The current market for cancer drugs worldwide is greater than $10.0 billion. Within this market, it is estimated that sales of drugs that inhibit mitosis, or anti-mitotic drugs, such as taxanes, most notably Taxol® from Bristol-Myers Squibb and Taxotere® from Sanofi-Aventis, comprise a large portion of the commercial market for cancer drugs. Worldwide sales from these taxanes alone represented over $2.0 billion in 2002. For Further Information Please Contact the Director of Business Development Michal Preminger Email: [email protected] Telephone: (617) 432-0920

Inventor(s): Mazitschek, Ralph

Type of Offer: Licensing



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