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Breakthrough Cancer Medication With Manifold Potency is Better Than Radiation

Update Date: Aug 30, 2012 09:00 AM EDT

In what could be termed as a major breakthrough in cancer medication, MU medicinal chemists have modified an existing cancer drug by adding a special structure to it and made it 10 times more potent in efficiently fighting the disease. 

"Over the past decade, we have seen an increasing interest in using carboranes in drug design," said Mark W. Lee Jr., assistant professor of chemistry in College of Arts and Science. "Carboranes are clusters of three elements-boron, carbon and hydrogen. Carboranes don't fight cancer directly, but they aid in the ability of a drug to bind more tightly to its target, creating a more potent mechanism for destroying the cancer cells." 

For the study, the researchers used carboranes in order to create a new drug designed to shut off the energy production of cancer cells, significant for the survival of it.

The energy produced by the cells is a complex and a multi-step process and in order to fight cancer, the drugs need to be able to target the process. 

If the binding strength of a drug is increased, only a smaller dose of it will be required, hence bringing down the side effects of the drug while increasing its effectiveness.

Lee found through the study that with carbonates the binding strength of the drug could be increased up to 10 folds. 

"The reason why these drugs bind stronger to their target is because carboranes exploit a unique and very strong form of hydrogen bonding, the strongest form of interactions for drugs," Lee said. 

Lee added that this finding could also pave way for more uses for the drug. 

"Too often, after radiation or chemotherapy, cancer cells repair themselves and reinvade the body," Lee said. "This drug not only selectively shuts off the energy production for the cancer cells, but it also inhibits the processes that allow those cancer cells to repair themselves. When we tested our carborane-based drugs, we found that they were unimaginably potent. So far, we have tested this on breast, lung and colon cancer, all with exceptional results." 

Lee further said that this is the first study of its kind to have systematically displayed how carboranes can improve the activity of a drug. 

"The end result is that these new drugs could be many thousands of times more potent than the drugs that are used in the clinics today," Lee said.

Although it might take years before the drug hits the market, the clinical trials should begin in the next two years, Lee said.

The study was published in the Journal of Medicinal Chemistry, a publication of the American Chemical Society.

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