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Updated: May 10, 2026

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
Published on: July 17, 2020
Protein tyrosine phosphatases as novel targets in breast cancer therapy
Caroline E Nunes-Xavier1, Jorge Martín-Pérez, Ari Elson
1BioCruces Health Research Institute, Hospital de Cruces, Plaza Cruces s/n, 48903 Barakaldo, Spain.
Abstract:
Breast cancer is linked to hyperactivation of protein tyrosine kinases (PTKs), and recent studies have unveiled that selective tyrosine dephosphorylation by protein tyrosine phosphatases (PTPs) of specific substrates, including PTKs, may activate or inactivate oncogenic pathways in human breast cancer cell growth-related processes. Here, we review the current knowledge on the involvement of PTPs in breast cancer, as major regulators of breast cancer therapy-targeted PTKs, such as HER1/EGFR, HER2/Neu, and Src. The functional interplay between PTKs and PTK-activating or -inactivating PTPs, and its implications in novel breast cancer therapies based on targeting of specific PTPs, are discussed.
Insights
Protein tyrosine phosphatases (PTPs) regulate protein tyrosine kinases (PTKs) in breast cancer. Understanding PTPs offers new therapeutic strategies targeting oncogenic pathways in breast cancer.
Area of Science:
- Oncology
- Biochemistry
- Molecular Biology
Background:
- Breast cancer is associated with hyperactivated protein tyrosine kinases (PTKs).
- Protein tyrosine phosphatases (PTPs) modulate PTK activity through dephosphorylation.
- PTPs play a critical role in regulating oncogenic pathways involved in breast cancer cell growth.
Purpose of the Study:
- To review the involvement of PTPs in breast cancer.
- To highlight PTPs as key regulators of targeted PTKs in breast cancer therapy.
- To discuss the implications of targeting PTPs for novel breast cancer treatments.
Main Methods:
- Literature review of current knowledge on PTPs and PTKs in breast cancer.
- Analysis of the functional interplay between PTPs and specific PTKs (e.g., HER1/EGFR, HER2/Neu, Src).
- Discussion of therapeutic strategies targeting PTPs in breast cancer.
Main Results:
- PTPs are major regulators of critical PTKs implicated in breast cancer.
- Selective dephosphorylation by PTPs can activate or inactivate oncogenic signaling pathways.
- The interplay between PTKs and PTPs is crucial for breast cancer progression.
Conclusions:
- PTPs are significant players in breast cancer pathogenesis.
- Targeting specific PTPs represents a promising avenue for novel breast cancer therapies.
- Further research into PTP-PTK interactions can lead to more effective breast cancer treatments.
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