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Updated: Feb 19, 2026
08:45
Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
Published on: July 17, 2020
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Therapeutic targeting of PP2A
Caitlin M O'Connor1, Abbey Perl1, Daniel Leonard2
1Department of Pharmacology, Case Western Reserve University, Cleveland, OH, 44106, United States.
The International Journal of Biochemistry & Cell Biology
|November 7, 2017
Summary
Protein phosphatase 2A (PP2A) is crucial for cellular functions and implicated in diseases like cancer. Therapeutic strategies targeting PP2A, including inhibitor management and direct targeting, are under investigation for clinical applications.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Protein phosphatase 2A (PP2A) is a key serine/threonine phosphatase regulating numerous cellular processes.
- PP2A's central role in biological functions and its dysregulation in diseases, particularly cancer, highlight its therapeutic potential.
Purpose of the Study:
- To review current therapeutic strategies targeting PP2A.
- To provide insight into the structural, molecular, and biological basis of PP2A-targeted therapies.
- To lay the groundwork for developing novel and clinically applicable PP2A-targeted treatments.
Main Methods:
- Review of existing literature on PP2A-directed therapeutics.
- Categorization of therapeutic approaches: inhibiting endogenous PP2A inhibitors, disrupting post-translational modifications, and direct PP2A targeting.
- Analysis of structural, molecular, and biological frameworks underlying therapeutic efficacy.
Main Results:
- Identified three primary categories of PP2A-directed therapeutic strategies.
- Highlighted the importance of understanding the underlying mechanisms for therapeutic development.
- Emphasized the need for further research into the efficacy and application of these strategies.
Conclusions:
- PP2A-directed therapies are a promising area of research for various diseases, especially cancer.
- A deeper understanding of PP2A's framework is essential for refining existing and developing new therapeutic interventions.
- Future research should focus on translating these insights into clinically tractable therapies.
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