Topoisomerase I Inhibitors Substituted with Carbohydrates

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Topoisomerase I is an ideal protein to target to reduce cancer activity given it is expressed more often in cancer cells than most terminally differentiated cells. The enzyme is responsible for structural changes in the DNA protein complex, allowing enzymes easy access for DNA synthesis. Topoisomerases have an important role in regulation of the cell cycle, and when the enzyme is inhibited from completing its task, the cell will activate death pathways. Many anticancer drugs have been designed to target this protein as it is expressed in all proliferating cells, which is a common feature of transformed cells. The problem with the synthesized drugs is they are not easily metabolized by the body and their insolubility makes them difficult to develop in the laboratory, limiting bioavailability.

Researchers at Purdue University have developed a new topoisomerase I inhibitor that incorporates carbohydrate groups to increase solubility. The result is drug that is more bioavailable and stable, which comes with the added benefit of smaller doses acting more effectively. The synthetic route developed for these compounds is simple, versatile, and easily scalable. The newly synthesized compounds displayed potent anti-Top1 activity and ceased proliferation in transformed cells.

-Carbohydrate-substituted indenoisoquinolines overcome common problems of solubility with this drug class
-Topoisomerase I is a proven target for cancer therapy

Potential Applications:
-Drug Development
-Cancer Treatment
May 2, 2016
United States
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May 25, 2011
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