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Updated: Jul 17, 2026
08:45
Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
Published on: July 17, 2020
Receptor Protein Tyrosine Phosphatases (RPTPs): Structure and Biological Roles in Cancer.
Abigail E Conklin1, Colin L Welsh2, Lalima K Madan1,3
1Department of Biochemistry and Molecular Biology, College of Medicine, Medical University of South Carolina, Charleston, SC 29425, USA.
Kinases and Phosphatases
|July 16, 2026
Summary
Receptor protein tyrosine phosphatases (RPTPs) are crucial in cancer, acting as tumor suppressors or promoters. Their roles vary by cancer type, highlighting RPTPs as potential therapeutic targets.
Area of Science:
- Biochemistry and Molecular Biology
- Cancer Research
- Signal Transduction
Background:
- Receptor protein tyrosine phosphatases (RPTPs) counteract protein tyrosine kinase activity, regulating key cellular processes.
- RPTPs are understudied compared to kinases, with emerging evidence of context-dependent roles in cancer.
- Their functions range from tumor suppression to promotion, influenced by tissue type and cellular context.
Purpose of the Study:
- To comprehensively review RPTP structure, mechanisms, regulation, and interactions in cancer.
- To analyze RPTP expression patterns across ten cancer types using proteogenomic data.
- To correlate expression alterations with functional classifications and therapeutic potential.
Main Methods:
- Systematic review of RPTPs in cancer.
- Analysis of RPTP expression data from Clinical Proteomic Tumor Analysis Consortium (CPTAC) and International Cancer Proteogenome Consortium (ICPC) datasets.
- Correlation of expression patterns with known functional roles (tumor suppressor/promoter).
Main Results:
- PTPσ and PTPμ are consistently downregulated tumor suppressors across multiple cancers.
- PTPα and PTPε demonstrate oncogenic potential by activating Src family kinases.
- Context-dependent RPTPs like LAR and DEP-1 show variable expression linked to complex signaling roles.
Conclusions:
- RPTPs are critical regulators of cancer signaling with significant therapeutic potential.
- Understanding tissue-specific signaling is essential for developing effective RPTP-targeted therapies.
- RPTP subfamily and cancer-type-specific expression alterations provide insights into their multifaceted roles in malignancy.
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