Related Experiment Video
Updated: Aug 25, 2026

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
Published on: July 17, 2020
Recent advances in protein tyrosine phosphatase 1B inhibitors
1Department of Chemistry, University of Waterloo, Ontario, Canada. s5taylor@sciborg.uwaterloo.ca
Abstract:
Type 2 diabetes and obesity are characterised by insulin and leptin resistance. Studies suggest that these may be due to defects in the insulin and leptin signalling pathways. Over the last decade, a considerable body of evidence has been amassed indicating that protein tyrosine phosphatase 1B (PTP1B) is involved in the downregulation of insulin and leptin signalling. Consequently, compounds that inhibit PTP1B have potential as therapeutics for treating Type 2 diabetes and obesity. This review covers recent advances in PTP1B inhibitors with an emphasis on recent attempts to create potent, selective and cell-permeable small-molecule inhibitors.
Insights
Protein tyrosine phosphatase 1B (PTP1B) inhibitors show promise for treating Type 2 diabetes and obesity by improving insulin and leptin signaling. Research focuses on developing potent, selective, and cell-permeable small-molecule inhibitors.
Area of Science:
- Biochemistry
- Pharmacology
- Metabolic Diseases
Background:
- Type 2 diabetes and obesity are linked to insulin and leptin resistance.
- Defects in insulin and leptin signaling pathways are implicated.
- Protein tyrosine phosphatase 1B (PTP1B) is known to downregulate these critical signaling pathways.
Purpose of the Study:
- To review recent advancements in the development of PTP1B inhibitors.
- To highlight strategies for creating potent, selective, and cell-permeable small-molecule inhibitors.
Main Methods:
- Literature review of recent research on PTP1B inhibitors.
- Analysis of studies focusing on small-molecule inhibitor design and properties.
Main Results:
- Evidence suggests PTP1B plays a key role in insulin and leptin resistance.
- Inhibitors of PTP1B are being developed as potential therapeutics.
- Focus is on achieving high potency, selectivity, and cell permeability in small-molecule inhibitors.
Conclusions:
- PTP1B inhibitors represent a promising therapeutic avenue for Type 2 diabetes and obesity.
- Continued research into small-molecule inhibitors is crucial for clinical translation.
Related Concept Videos
Protein Kinases and Phosphatases
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Phosphoinositides and PIPs
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...
PI3K/mTOR/AKT Signaling Pathway
Receptor Tyrosine Kinases

