Related Experiment Video
Updated: Jun 26, 2026

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
Published on: July 17, 2020
Phosphatases of regenerating liver downregulate PTEN to promote tumorigenesis
Ahmed M Abou-Shanab1,2, Jingmei Yu1, Yunpeng Bai1
1Borch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, 720 Clinic Drive, West Lafayette, IN 47907, U.S.A.
Abstract:
The phosphatase and tensin homolog deleted on chromosome 10 (PTEN) is one of the most frequently inactivated tumor suppressors in human cancers, serving as a critical negative regulator of phosphatidylinositol 3-kinase (PI3K)-AKT signaling. Although genetic mutation or deletion commonly underlie functional PTEN loss, accumulating evidence indicates that post-transcriptional and post-translational mechanisms also substantially contribute to PTEN suppression. Phosphatases of regenerating liver (PRLs), comprising PRL1, PRL2, and PRL3, are oncogenic phosphatases frequently overexpressed in both solid and hematological malignancies. Emerging studies reveal that PRLs can downregulate PTEN through a post-translational mechanism by direct dephosphorylation of PTEN at Tyr336, therefore promoting PTEN ubiquitination and proteasomal degradation. PRLs can also reduce PTEN expression through a post-transcriptional mechanism by dephosphorylating the inhibitory Tyr570 in JAK2, thereby activating the JAK2/STAT3-mediated miR-21 expression. These coordinated actions collectively amplify PI3K-AKT signaling, consequently promoting proliferation, survival, and metastasis. In the present review, we synthesize current knowledge of PRL structure, evolution, and functional diversity, evaluate genetic, biochemical, and organismal evidence linking PRLs to PTEN regulation, and discuss insights on PRL oncogenicity derived from experimental models. We further examine context-dependent functions of PRLs, unresolved questions regarding catalytic versus scaffold activities, and the therapeutic potential of targeting the PRL-PTEN axis. Understanding how PRLs modulate PTEN activity may reveal new strategies to restore tumor suppressor function in PTEN-deficient cancers.
Insights
Phosphatases of regenerating liver (PRLs) suppress the tumor suppressor PTEN through post-translational and post-transcriptional mechanisms. This review synthesizes evidence on PRLs, PTEN regulation, and therapeutic strategies targeting the PRL-PTEN axis in cancer.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- PTEN is a critical tumor suppressor frequently lost in cancers.
- PRLs are oncogenic phosphatases overexpressed in various malignancies.
- PTEN loss can occur via post-transcriptional and post-translational mechanisms.
Purpose of the Study:
- To review the structure, evolution, and functional diversity of PRLs.
- To evaluate evidence linking PRLs to PTEN regulation.
- To discuss the therapeutic potential of targeting the PRL-PTEN axis.
Main Methods:
- Literature review synthesizing genetic, biochemical, and organismal evidence.
- Analysis of experimental models to understand PRL oncogenicity.
- Examination of PRL structure, evolution, and functional diversity.
Main Results:
- PRLs downregulate PTEN via direct dephosphorylation (post-translational) and JAK2/STAT3/miR-21 pathway (post-transcriptional).
- These actions amplify PI3K-AKT signaling, promoting cancer progression.
- PRLs exhibit context-dependent functions and catalytic/scaffold activities.
Conclusions:
- PRLs are key regulators of PTEN, contributing to oncogenesis.
- Targeting the PRL-PTEN axis offers potential therapeutic strategies for PTEN-deficient cancers.
- Further research into PRL functions may reveal novel cancer treatments.
Related Concept Videos
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
PI3K/mTOR/AKT Signaling Pathway
Abnormal Proliferation
Liver Regeneration
Cells of Liver
The liver comprises four major types of cells— hepatocytes, stellate, Kupffer, and sinusoidal endothelial cells. The hepatocytes are large...
Negative Regulator Molecules
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...