Development of novel protein tyrosine phosphatase - 1B (PTP1B) inhibitors to enhance insulin cell signaling
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چکیده
Diabetes mellitus is a primary cause for large number of pathophysiologic co-morbidities including obesity, hypertension, hyperlipidemia, atherosclerosis. Obesity is intimately associated with diabetes, which is not only a major but also a costly healthcare problem for the individual and to the society. The World Health Organization (WHO) estimates that approximately 135 million people worldwide currently have diabetes and in that type II diabetes accounts for around 90% and it will rise up to two fold by the year 2025. To manage diabetes and diabetes linked abnormalities wide variety of therapeutic agents including combination therapy are now being used. Targeting blood glucose level without disturbing lipid metabolism becomes more difficult to maintain with monotherapy. Even worse the current anti-diabetic therapy promotes weight gain i.e. obesity, while reducing blood glucose (eg. Thiazolidinediones and Sulphonylureas). Botanicals are thought of offering strong potential with minimal side affects particularly against metabolic syndromes as most of their efficacies are from a mixture of active molecules acting at the same time. By understanding the potential of medicinal plants and the expanding diabetic population it is highly desirable to find anti diabetic agents that regulate glucose metabolism without disturbing lipid metabolism with complete mechanism of action, safety and quality profile.
منابع مشابه
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Protein tyrosine phosphatase 1B (PTP1B) is a key negative regulator of insulin signaling pathway. Inhibition of PTP1B is expected to improve insulin action. Appropriate selectivity and permeability are the gold standard for excellent PTP1B inhibitors. In this work, molecular hybridization-based screening identified a selective competitive PTP1B inhibitor. Compound 10a has IC50 values of 199 nM ...
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تاریخ انتشار 2011