Cancer Drugs Can Be Made More Potent
August 30, 2012

Carboranes Help Boost Cancer Drug Effectiveness

Watch the Video: MU Research Team Creates Potent Cancer Drug

Lee Rannals for - Your Universe Online

Medicinal chemists have rolled up their sleeves and created a new cancer drug that is 10 times as potent as current drugs.

The team set out to take an existing drug being developed to fight certain cancers, added special structures to it, and created an even more powerful weapon to combat the deadly affliction.

"Over the past decade, we have seen an increasing interest in using carboranes in drug design," according to Mark W. Lee Jr., assistant professor of chemistry in College of Arts and Science at the University of Missouri-Columbia.

"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."

During the study, the team used carboranes to build new drugs designed to shut off a cancer cell's energy production. Increasing the binding strength of a drug minimizes side effects, and increases the effectiveness of the therapy.

The team found that carboranes helped to make the drug bind 10 times more powerfully than before.

"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.

He also said that this discovery will also lead to further uses for the drug.

"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," Lee said. "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."

The researcher added that this is the first study to show systematically how carboranes can improve the activity of a drug.

He believes this discovery will open up more possibilities of improving drugs that are used to treat other diseases.

"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.

Clinical trials could being within the next two years, but it could take several years before the new drug would be available.

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