Development of a lead boron-containing ClpP inhibitor for AML therapy

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Cancer continues to be one of the leading causes of death in the world. This disease is exceptionally complex, which is why it is extremely important to evaluate different angles for therapeutic intervention. This area of modern science involves a number of disciplines, of which chemistry and biology play central roles. While biologists continue to discover new molecular targets that make cancer cell susceptible to treatment, chemists are busy using the results of these studies in order to prepare molecules that can kill cancer cells. The present grant proposal combines the efforts of a renowned cancer hematologist (Schimmer) and a well-known expert in synthetic chemistry (Yudin). Together, the Schimmer and Yudin labs had realized that some of the molecules recently prepared in the Yudin lab can be particularly effective in killing the cancer cells under investigation in the Schimmer lab. As a proof of concept, the two teams were able to show that boron-containing molecules developed by Yudin and his students are particularly well suited to attack proteins that are thought to be present in leukaemia cells. We plan to capitalize on our exciting preliminary results and ensure that our molecules are translated into a clinical asset. In the course of this study, we will also be able to evaluate the significance of our chosen target in cancer therapy. Encouragingly, we have been able to attract interest on behalf of well-known companies (Merck, AstraZeneca, and Anacor), who will help us in our search of effective anti-cancer therapeutics.