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Protein Kinases and Phosphatases

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Updated: May 11, 2026

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors

Published on: July 17, 2020

Protein phosphatase 2A: a target for anticancer therapy.

Danilo Perrotti¹, Paolo Neviani

¹Human Cancer Genetics Program, Department of Molecular Virology, Immunology, and Medical Genetics, and Comprehensive Cancer Center, Ohio State University, Columbus, OH 43210-2207, USA. danilo.perrotti@osumc.edu

The Lancet. Oncology

|May 4, 2013

Summary

Protein phosphatase 2A (PP2A) is a tumor suppressor enzyme crucial for cell homeostasis. Restoring PP2A activity with drugs shows promise in combating cancer development and progression.

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Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors

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A Mass Spectrometry-Based Approach to Identify Phosphoprotein Phosphatases and their Interactors

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Published on: April 29, 2022

Area of Science:

Molecular Biology
Cellular Biology
Oncology

Background:

Protein phosphatase 2A (PP2A) is a key serine-threonine phosphatase regulating cellular homeostasis.
PP2A activity is often inhibited in various cancers, contributing to oncogenic kinase signaling.
PP2A functions as a tumor suppressor, counteracting pro-cancerous pathways.

Purpose of the Study:

To discuss the role of PP2A as a druggable target in cancer therapy.
To explore the potential of PP2A-activating drugs in anticancer treatment protocols.

Main Methods:

Literature review and discussion of existing preclinical data.
Analysis of PP2A's function in cancer development and progression.

Main Results:

PP2A inactivation is implicated in numerous solid cancers and leukaemias.
Pharmacological activation of PP2A demonstrates efficacy in preclinical cancer models.
PP2A-activating drugs, such as FTY720, can antagonize cancer progression.

Conclusions:

PP2A is a validated tumor suppressor with significant therapeutic potential.
PP2A-activating drugs represent a promising strategy for future anticancer protocols.