Protein Tyrosine Phosphatase 1B inhibitors

What is it about?

The major currently available management strategies are sulfonylureas, biguanides, thiazolidinediones, α-glucosidase inhibitors, dipeptidyl peptidase-IV inhibitors, and glucagon-like peptide-1 (GLP-1) agonist. Binding of insulin on the extracellular unit of insulin receptor sparks tyrosine kinase of insulin receptor and which induces autophosphorylation. The phosphorylation of the tyrosine is regulated by insulin and leptin molecules. Protein tyrosine phosphatase-1B (PTP1B) works as a negative governor for the insulin signalling pathways, as it dephosphorylates the tyrosine of insulin receptor and suppress the insulin signalling cascade. The compounds or molecules which inhibit the negative regulation of PTP1B can have an inducive effect on the insulin pathway and finally helps in the management of diabetes mellitus. PTP1B could be an emerging therapeutic strategy for the diabetes management.

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Why is it important?

Diabetes is one of the most common endocrine non-communicable metabolic disorder which is mainly caused either due to insufficient insulin or inefficient insulin or both together and is characterised by hyperglycemia. Diabetes emerged as a serious health issue in industrialized and developing country specially in Asian pacific region. Out of two major category of diabetes mellitus, type 2 diabetes is more prevalent, almost 90 to 95% cases, and the main cause of this is insulin resistance. The main cause of the progression of type 2 diabetes mellitus has been found to be the insulin resistance. The type 2 diabetes mellitus may be managed by the change in life style, physical activities, dietary modifications and medications.

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