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Updated: Jun 5, 2026

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
Published on: July 17, 2020
Inside the human cancer tyrosine phosphatome
Sofi G Julien1, Nadia Dubé, Serge Hardy
1Goodman Cancer Research Centre, Department of Biochemistry, McGill University, Montreal, Quebec, Canada.
Abstract:
Members of the protein tyrosine phosphatase (Ptp) family dephosphorylate target proteins and counter the activities of protein tyrosine kinases that are involved in cellular phosphorylation and signalling. As such, certain PTPs might be tumour suppressors. Indeed, PTPs play an important part in the inhibition or control of growth, but accumulating evidence indicates that some PTPs may exert oncogenic functions. Recent large-scale genetic analyses of various human tumours have highlighted the relevance of PTPs either as putative tumour suppressors or as candidate oncoproteins. Progress in understanding the regulation and function of PTPs has provided insights into which PTPs might be potential therapeutic targets in human cancer.
Insights
Protein tyrosine phosphatases (PTPs) counteract kinases in cell signaling. While some PTPs act as tumor suppressors, others promote cancer, highlighting their complex roles and potential as therapeutic targets.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Protein tyrosine phosphatases (PTPs) are enzymes that remove phosphate groups from proteins.
- PTPs counteract the action of protein tyrosine kinases (PTKs), which are involved in cellular signaling pathways.
- The role of PTPs in cancer is complex, with some acting as tumor suppressors and others as oncogenes.
Purpose of the Study:
- To review the dual role of PTPs in cancer.
- To highlight the significance of PTPs in human tumors based on recent genetic analyses.
- To discuss the potential of PTPs as therapeutic targets in cancer treatment.
Main Methods:
- Literature review of recent large-scale genetic analyses of human tumors.
- Analysis of existing research on PTP regulation and function in cancer.
- Synthesis of evidence regarding the oncogenic and tumor-suppressive roles of PTPs.
Main Results:
- PTPs play a critical role in regulating cell growth and signaling.
- Genetic analyses reveal PTPs are frequently implicated in various human cancers.
- Evidence supports both tumor-suppressive and oncogenic functions for different PTP members.
Conclusions:
- PTPs are key regulators of cellular processes relevant to cancer.
- Understanding the specific roles of PTPs in different cancers is crucial.
- PTPs represent promising therapeutic targets for cancer intervention.
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