Status of research on natural protein tyrosine phosphatase 1B inhibitors as potential antidiabetic agents: Update

Protein tyrosine phosphatase 1B (PTP1B) is a crucial therapeutic target for multiple human diseases comprising type 2 diabetes (T2DM) and obesity because it is a seminal part of a negative regulator in both insulin and leptin signaling pathways. PTP1B inhibitors increase insulin receptor sensitivity and have the ability to cure insulin resistance-related diseases. However, the few PTP1B inhibitors that entered the clinic (Ertiprotafib, ISIS-113715, Trodusquemine, and JTT-551) were discontinued due to side effects or low selectivity. Molecules with broad chemical diversity extracted from natural products have been reported to be potent PTP1B inhibitors with few side effects. This article summarizes the recent PTP1B inhibitors extracted from natural products, clarifying the current research progress, and providing new options for designing new and effective PTP1B inhibitors.

Automated summary

Protein tyrosine phosphatase 1B (PTP1B) is an important therapeutic target for diseases such as type 2 diabetes and obesity. PTP1B inhibitors have the potential to improve insulin receptor sensitivity and treat insulin resistance-related diseases. However, the currently available PTP1B inhibitors have been discontinued due to side effects or low selectivity. This article summarizes recent research on PTP1B inhibitors extracted from natural products and provides new options for designing effective inhibitors.