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Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
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Druggable cancer phosphatases

Julia P Vainonen1, Majid Momeny1, Jukka Westermarck2,3

  • 1Turku Bioscience Centre, University of Turku and Åbo Akademi University, 20520 Turku, Finland.

Science Translational Medicine
|April 8, 2021
PubMed

Insights

Targeting phosphatases, enzymes regulating protein phosphorylation, offers new cancer treatment strategies. This review highlights progress in developing drugs against oncogenic SHP2 and tumor suppressor PP2A phosphatases for improved cancer therapies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Protein phosphorylation, crucial for cell signaling, is dysregulated in cancer.
  • Phosphatases, key regulators of phosphorylation, have been historically challenging drug targets.
  • Emerging strategies now focus on targeting specific phosphatases for cancer therapy.

Purpose of the Study:

  • To review therapeutic targeting of oncogenic and tumor suppressor phosphatases in cancer.
  • To discuss small molecules targeting phosphatases like SHP2 and PP2A.
  • To explore advances in clinical development and combination therapies.

Main Methods:

  • Literature review of pharmacological approaches targeting phosphatases.
  • Analysis of small molecules targeting SHP2 and PP2A.
  • Examination of clinical trial data and combination strategies.

Main Results:

  • SHP2 and PP2A are identified as druggable phosphatases with therapeutic potential.
  • Various small molecules targeting these phosphatases are in development.
  • Combination therapies show promise for enhanced efficacy.

Conclusions:

  • Targeting phosphatases represents a promising frontier in cancer drug development.
  • SHP2 and PP2A inhibitors are advancing through clinical trials.
  • Innovative pharmacological strategies are expanding treatment options for cancer patients.

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