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Updated: Oct 14, 2025

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
Published on: July 17, 2020
Recent advances in PTP1B signaling in metabolism and cancer
Olga Villamar-Cruz1,2, Marco A Loza-Mejía3, Luis E Arias-Romero2
1Unidad de Investigación en Reproducción Humana, Instituto Nacional de Perinatología-Facultad de Química, Universidad Nacional Autónoma de México (UNAM), Ciudad de México, Mexico.
Abstract:
Protein tyrosine phosphorylation is one of the major post-translational modifications in eukaryotic cells and represents a critical regulatory mechanism of a wide variety of signaling pathways. Aberrant protein tyrosine phosphorylation has been linked to various diseases, including metabolic disorders and cancer. Few years ago, protein tyrosine phosphatases (PTPs) were considered as tumor suppressors, able to block the signals emanating from receptor tyrosine kinases. However, recent evidence demonstrates that misregulation of PTPs activity plays a critical role in cancer development and progression. Here, we will focus on PTP1B, an enzyme that has been linked to the development of type 2 diabetes and obesity through the regulation of insulin and leptin signaling, and with a promoting role in the development of different types of cancer through the activation of several pro-survival signaling pathways. In this review, we discuss the molecular aspects that support the crucial role of PTP1B in different cellular processes underlying diabetes, obesity and cancer progression, and its visualization as a promising therapeutic target.
Insights
Protein tyrosine phosphatase 1B (PTP1B) is crucial in regulating cell signaling. This enzyme links to type 2 diabetes, obesity, and cancer, highlighting its potential as a therapeutic target.
Area of Science:
- Molecular Biology
- Cellular Signaling
- Biochemistry
Background:
- Protein tyrosine phosphorylation is a key post-translational modification regulating eukaryotic cell signaling.
- Aberrant phosphorylation is implicated in metabolic disorders and cancer.
- Protein tyrosine phosphatases (PTPs), once viewed as tumor suppressors, are now recognized for their critical role in cancer progression.
Purpose of the Study:
- To review the molecular mechanisms of PTP1B in diabetes, obesity, and cancer.
- To highlight PTP1B's role in insulin and leptin signaling.
- To discuss PTP1B as a therapeutic target.
Main Methods:
- Literature review of molecular and cellular studies.
- Analysis of signaling pathways regulated by PTP1B.
- Examination of PTP1B's role in disease pathogenesis.
Main Results:
- PTP1B regulates insulin and leptin signaling, linking it to type 2 diabetes and obesity.
- PTP1B promotes cancer development by activating pro-survival pathways.
- Misregulation of PTP1B activity is critical in cancer progression.
Conclusions:
- PTP1B plays a significant role in cellular processes underlying diabetes, obesity, and cancer.
- PTP1B is a promising therapeutic target for these diseases.
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