Scientists have developed a safer drug that can replace potentially the insulin jabs or diabetes needles that the patients undergo almost daily once they are diagnosed with the slow-killer disease.
Instead of traditional Metformin drug, the new drug targets a protein receptor known as PPARgamma found in fat tissue throughout the body, by activating it to achieve lower blood sugar in Type 2 diabetes treatment.
Research led by the University of Adelaide, published in the Journal of Medicinal Chemistry, shows for the first time how new potential anti-diabetic drugs interact with their target in the body at the molecular level.
“Type two diabetes is characterised by resistance to insulin with subsequent high blood sugar which leads to serious disease. It is usually associated with poor lifestyle factors such as diet and lack of exercise,” says lead researcher Dr John Bruning, with the University’s School of Biological Sciences and Institute for Photonics and Advanced Sensing.
Despite insulin injections, it’s difficult to get insulin levels just right and hence, the new use of oral therapeutics, argue the Australian researchers.
The first study done at the Scripps Research Institute in Florida, US, found 14 different versions of a drug which partially activates PPARgamma with the benefit of fewer side-effects and their drug INT131 is currently being tested in clinical trials in the US.
However, some of the versions produced at the University of Adelaide have increased potency compared to the original, with the potential to further improve the treatment of type 2 diabetes.
“A major finding of this study was being able to show which regions of the drug are most important for interacting with the PPARgamma receptor,” says Dr Bruning. “This means we now have the information to design modified drugs which will work even more efficiently.”
The second study, in collaboration with Flinders University, used X-ray crystallography to demonstrate for the first time exactly how a potential new drug, rivoglitazone, binds with the PPARgamma receptor. Rivoglitazone fully activates PPARgamma but has less side effects than others with this mode of action.