The team of specialists provided a research on the role of Gleevec in the treatment of insulin resistance and type 2 diabetes. This study was published in the journal Diabetes in 2016 and presents a new intervention for the treatment of type 2 diabetes in adults and children. The main problem is that obesity is widespread nowadays, it results in diabetes, dyslipidemia, hypertension, and cardiovascular diseases. The key idea is that Gleevec can be a novel therapeutic agent for use in insulin resistance and type 2 diabetes only if its potential adverse effects will be removed (Choi 2016). However, the team of specialists managed to remove the negative impact of Gleevec and suggest that it can be successfully used in treatment of obesity and type 2 diabetes.
Diabetes is a complex heterogeneous disease that is rarely diagnosed without a special blood test. According to statistics, nearly 370 million people suffer from diabetes, and half of them do not know about this disease. Diabetes is a disease of the endocrine system caused by absolute or relative insulin deficiency, characterized by a chronic increase in blood sugar level.
It is a serious medical and social problem of almost all countries of the world and there is a trend to an increase in the incidence of diabetes. Currently, there are many pharmacological agents that cause concern about their potential side effects and the possible impact on patients. Thus, when the doctor gets the choice to provide hypoglycemic therapy, he should be clearly aware of all the options of modern treatment, the advantages, and disadvantages of all groups of products on the market (Choi 2016).
The team of specialists revealed that thiazolidinediones (TZDs) has been used for the treatment of type 2 diabetes. Its use often results in negative side effects such as weight gain, fluid retention, bone fracture, cardiovascular disease, and bladder cancer. Thus, the use of such medication for the treatment of type 2 diabetes was restricted. From the other side, PPARγ is connected with obesity and insulin resistance. Its Ps273 is important for the development of antidiabetes drugs. The team of researchers considered this topic and found that Gleevec is an anticancer drug that blocks PRARy phosphorylation, contributes to insulin sensitivity, regulates glucose production and proinflammatory responses. Such properties have antiobesity effects that suggest that Gleevec can be used in the treatment of diabetes and obesity (Choi 2016). However, negative side effects should be removed.
Animal experiments were provided to prove a suggestion. Animals were injected with Gleevec for 7 days, with D-glucose. Then they passed insulin tolerance tests, their body temperatures were measured, blood glucose levels were determined. The data obtained indicated positive impact of f Gleevec on glucose metabolism, but the molecular and cellular mechanisms remain unclear. Gleevec inhibited PPARγ phosphorylation but didn’t inhibit the CDK5-mediated phosphorylation of retinoblastoma. It was found that Gleevec targets PRARy and inhibits pS273. A team of scientists concluded that Gleevec specifically blocks pS273, independent of its BCR-Abl targeting.
It is widely believed that obesity is closely linked to chronic low-grade inflammation that contributes to the development of insulin resistance. Thus, a direct impact on inflammation in adipose tissue can have positive outcomes for treatment of inflammatory responses in obesity.
They also studied whether pS273 of PPARγ is involved in the anti-inflammatory activity in adipocytes and M2 polarization in macrophages. Obtained results indicate that blocking pS273 by Gleevec ameliorates adipose inflammation. PRARy also impacts energy balance by promoting browning of WAT (Choi 2016).
PPARγ ligands and TZDs were widely used to treat type 2 diabetes. Unfortunately, patients experienced adverse effects compared with other medications. In order to deal with such effects, studies indicated that insulin-sensitizing effects of PPARγ ligands are a result of ligand-dependent inhibition of pS273 by CDK5/ERK kinases. Also, nonagonist PPARγ ligands demonstrated treatment effects similar to TZDs but they didn’t have any negative effects. Such results allow to provide a research to find the new treatment of type 2 diabetes. Gleevec is an anticancer drug that has dramatic effects for CML and gastrointestinal stromal tumors, has a blood glucose-lowering effect and can be used for treatment without side adverse effects or another negative impact (Choi 2016).
The present study revealed that Gleevec has a great potential to regulate glucose and lipid metabolism even without adverse effects. The main idea is that it promotes the development of being fat in WAT, and Gleevec plays an important role in the treatment of obesity and type 2 diabetes. This research can be used in practice as it describes a work of Gleevec, its impact on insulin sensitivity, gene expression in liver, impact on white adipose tissue and energy expenditure. The team of researchers resolved a problem of unwanted side effects of the use of TZDs, which use was restricted by the U.S. Food and Drug Administration (FDA) for the treatment of type 2 diabetes (Choi 2016). The present results indicate that Gleevec can effectively treat obesity and type 2 diabetes.
References
Choi, C. et.al. (2016). PPARγ Antagonist Gleevec Improves Insulin Sensitivity and Promotes the Browning of White Adipose Tissue. Diabetes, 65(8). Web. 20 August 2016.
