TSRI scientist receives $2.1M grant to study therapeutic potential of alternatives to current crop of anti-diabetic drugs

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Scientists from the Florida campus of The Scripps Research Institute (TSRI) have been awarded $2.1 million from the National Institutes of Health to study the therapeutic potential of safer and more effective alternatives to the current crop of anti-diabetic drugs, which have been limited in their use due to side effects including bone loss and congestive heart failure.

Douglas Kojetin, a TSRI associate professor, is the principal investigator for the new five-year study.

The study will take a cue from the two mainstays of type 2 diabetes treatment-pioglitazone (Actos) and rosiglitazone (Avandia). Both drugs raise the body's sensitivity to insulin, increasing the amount of glucose or sugar absorbed by the cells.

Studies have shown, however, that while these and other recently developed drugs are designed to bind to a specific site on the PPAR gamma (PPARG) nuclear receptor, they can also bind to an alternative site.

"This unexpected finding opens a lot of potential opportunities," Kojetin said. "We're looking to design a molecule that blocks both sites and can be used to probe what this alternative binding does on a molecular level-with the hope that this information will help us come up with a better drug model."


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