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Updated: Jun 24, 2026
08:45
Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
Published on: July 17, 2020
Targeting protein serine/threonine phosphatases for drug development
Jamie L McConnell1, Brian E Wadzinski
1Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232-6600, USA.
Molecular Pharmacology
|March 21, 2009
Summary
Protein phosphatases are emerging therapeutic targets. This review explores their role in disease, highlighting successes and challenges in developing drugs that modulate their activity for better cellular signaling.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Recent clinical success of protein kinase inhibitors has shifted focus to other enzymes in signaling pathways.
- Reversible protein phosphorylation plays a critical role in various disease states.
- Protein phosphatases counteract protein kinases and are key regulators of cellular signaling.
Purpose of the Study:
- To review protein serine/threonine phosphatases as potential therapeutic targets.
- To discuss the current landscape of modulating phosphatase activity for disease treatment.
- To outline future strategies for drug discovery targeting these enzymes.
Main Methods:
- Literature review of existing research on protein phosphatases.
- Analysis of past therapeutic successes and challenges.
- Discussion of current and future strategies for drug development.
Main Results:
- Protein serine/threonine phosphatases represent viable targets for therapeutic intervention.
- Modulating phosphatase activity offers a promising approach to alter cellular signaling.
- Significant challenges remain in developing effective phosphatase-modulating drugs.
Conclusions:
- Protein phosphatases are crucial targets for drug discovery.
- Further research is needed to overcome challenges in developing phosphatase inhibitors or activators.
- Targeting phosphatases holds potential for treating a range of diseases.
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