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New compounds may treat both diseases and diabetes

2017-02-22 来源:转载自第三方
22 February 2017
  Researchers from the University of Bath in UK and the University of Oulu in Finland have recently created a new compound molecule that can increase adipocyte glucose intake and inhibit the growth of colon cancer cells, and is expected to be used in the future for the treatment of cancer and diabetes. The study was published in the <Journal of Medicinal Chemistry>, entitled "Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity" [1].
Figure 1. New research published in JMC.
  Diabetes is a comprehensive metabolic diseases. According to hypoglycemic mechanism, the current treatment of drugs can be divided into the following categories: sulfonylureas, such as glibenclamide, glimepiride, etc.; biguanides, such as phenformin, Metformin; α-glucosidase inhibitors such as acarbose, voglibose; insulin sensitizers such as rosiglitazone, troglitazone and so on; GLP-1 receptor agonists Exenafil ; DPP-4 inhibitor vildagliptin (intermediate 3-amino-1-adamantanol), etc.; and various types of insulin. The occurrence and development of colon cancer is the result of multi-gene and multi-incident accumulation. After many years of research, it has been found that Wnt signaling pathway is involved in the pathogenesis of human colorectal cancer. At present, there is no drug to be able to treat both diseases at the same time.
  In this study, Researchers at the University of Bath collaborated with researchers of the University of Oulu specifically characterize two molecules that inhibit TNKS with 8-aminoquinoline as a substrate. This molecule plays an important role in the Wnt/β-catenin signaling pathway, which enhances the adipocyte glucose intake and inhibits proliferation of colon cancer cells. The compound is expected to be a drug for simultaneous treatment of cancer and diabetes.
Figure 2. Crystal structures of two compounds that bind to the TNKS [1].
  Although it is too early to talk about the new molecule of drugs that can treat both diabetes, colon cancer and other inflammatory tumors at the same time, but it is an important start. The next step, the researchers will further optimize the compound molecules, and use a specific model to assess its efficacy, further study the opportunity to develop possible treatment programs. They plan to use cancer cells to develop a 3D model to better understand TNKS/Wnt signaling pathway inhibitors; while using obesity and diabetes to investigate the biological model of fat cell reduction and insulin sensitivity.
  According to the data from International Diabetes Federation, there are more than 450 million people suffering from diabetes at present, by 2025, there will be about 175 million patients worldwide, by 2040, there will be about 642 million patients, diabetes easily lead to obesity, cardiovascular disease and other complications; and cancer will also affect the function of the body system, a better treatment than surgery and chemotherapy will give patients reat benefits in body and spirit. Therefore, the development of drugs that can treat both diseases at the same time is of great significance to both society and patients.
[1] Amit Nathubhai, Teemu Haikarainen, Jarkko Koivunen, et al. Highly Potent and Isoform Selective Dual Site Binding Tankyrase / Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity. J. Med. Chem., 2017, 60 (2 ), pp. 814-820.
Related Links: 3-Amino-1-adamantanol
1,1-Dimethylbiguanide hydrochloride
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