The Cancer Silver Bullet ‘Gleevec’ is Promising in Type II Diabetes
Imatinib, marketed by Novartis as Gleevec is tyrosine-kinase inhibitor and often consider as silver bullet in certain cancer therapy is now reported to have a new and promising pharmacology in the treatment for Type II diabetes.
The research were carried out on mice in which gleevec lowered the levels of insulin and also reduced the risks of hyperglycemia and obesity without causing severe side effects. The results of the research were covered in a report published in the journal diabetes by a team of Korean scientists. The report also revealed that the effects of gleevec on insulin sensitivity and blood sugar levels were similar to another group of drugs called thiazolidinediones (TZD). It is to be noted that TZDs were removed from the market after increased incidences of side effects including increased risks of heart attack.
TZDs are a group of drugs that block the transcription factor PPARγ (peroxisome proliferator-activated receptors), which is required for the metabolism of glucose and the phosphorylation of PPARγ is related to the development of diabetes. It was also discovered that the removal of phosphoric acid from PPARγ shows anti-diabetic effects. A team comprising of scientists from Scripps Research Institute in the US, South Korean company Hyundai Pharm Co, Ulsan National Institute of Science and Technology and Seoul National University, Korea found that gleevec can inhibit the phosphorylation of PPARγ by blocking Cdk5 factor and thus treat type II Diabetes. They further reported that gleevec lowers Insulin resistance thus decreasing risks of hyperglycemia and obesity.
“Although studies have shown that Gleevec treatment may show improved insulin sensitivity and decrease blood glucose in patients with known diabetes, the exact cause hasn’t been proven yet,” Jang Hyun Choi, a professor in the school of life sciences at the Ulsan National Institute of Science and Technology, said in a press release. “Through this research, we discovered Gleevec, which is used in leukemia medications, can inhibit the phosphorylation of PPARγ.”
According to report, taken together, gleevec exhibits greater beneficial effects on both glucose/lipid metabolism and energy homeostasis by blocking PPARγ phosphorylation, and thus these data illustrate that gleevec could be a novel therapeutic agent for use in insulin resistance and type 2 diabetes. In the study, researchers also found that gleevec showed improved insulin sensitivity in mice fed high-fat diets, without severe side effects. The drug also reduced lipogenic and gluconeogenic gene expression in the liver, and improved inflammation in adipose tissue, all of which the researchers said are useful against Type II diabetes.
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