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Updated: Jul 6, 2025

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
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Altering phosphorylation in cancer through PP2A modifiers.

Hannah Johnson1, Satya Narayan2, Arun K Sharma3

  • 1Department of Pharmacology, Penn State Cancer Institute, The Pennsylvania State University College of Medicine, Hershey, PA, 17033, USA.

Cancer Cell International
|January 6, 2024
PubMed
Summary
This summary is machine-generated.

Protein phosphatase 2A (PP2A) is crucial for cellular processes. Deregulation of PP2A in cancer promotes tumor growth, making PP2A inhibitors and activators promising therapeutic strategies.

Keywords:
ActivatorsCancerInhibitorsPP2ATherapeutics

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Protein phosphatase 2A (PP2A) is a key serine/threonine phosphatase regulating numerous cellular functions.
  • PP2A dysregulation is implicated in cancer progression, driving tumor growth.
  • Targeting PP2A offers a therapeutic avenue for cancer treatment.

Purpose of the Study:

  • To review the role of PP2A in cancer.
  • To discuss PP2A's downstream signaling pathways in cancer regulation.
  • To explore PP2A activators and inhibitors as anti-cancer agents.

Main Methods:

  • Literature review of PP2A deregulation in cancer.
  • Analysis of PP2A's role in cancer signaling pathways.
  • Compilation of known PP2A modulators (activators and inhibitors).

Main Results:

  • PP2A deregulation contributes to tumor progression.
  • PP2A modulators demonstrate efficacy in various cancers, including drug-resistant types.
  • PP2A targeting can synergize with existing cancer therapies.

Conclusions:

  • PP2A is a significant target for cancer therapy.
  • Modulating PP2A activity through inhibitors or activators can impede cancer progression.
  • PP2A-targeted therapies hold promise for overcoming drug resistance and enhancing treatment efficacy.