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The Therapeutic Potential of PTEN Modulation: Targeting Strategies from Gene to Protein

Niall M McLoughlin1, Carolin Mueller1, Tom N Grossmann2

  • 1Department of Chemistry and Pharmaceutical Sciences, VU University Amsterdam, 1081 HZ Amsterdam, the Netherlands.

Cell Chemical Biology
|November 21, 2017
PubMed

Insights

PTEN, a tumor suppressor, has complex roles in cancer and neuroregeneration. New strategies are needed to modulate PTEN

Area of Science:

  • Molecular Biology
  • Oncology
  • Neuroscience

Background:

  • The tumor suppressor Phosphatase and TENsin homolog (PTEN) was discovered two decades ago.
  • PTEN has diverse biological functions, with potential therapeutic applications in cancer and neuroregeneration.
  • PTEN's "risky" tumor suppressor profile complicates its therapeutic use.

Purpose of the Study:

  • To evaluate PTEN function and its roles in disease.
  • To summarize current PTEN-targeting strategies.
  • To discuss potential approaches for modulating PTEN's functional dose.

Main Methods:

  • Review of existing PTEN-targeting molecules and strategies.
  • Analysis of challenges in PTEN modulation, including phosphatase inhibition and post-translational modifications.
  • Consideration of PTEN biogenesis stages: gene, mRNA, protein, and miRNA regulation.

Main Results:

  • Development of various molecules to evaluate PTEN function and disease roles.
  • Intrinsic challenges hinder straightforward access to selective PTEN modulators.
  • Central questions regarding PTEN targeting remain unanswered.

Conclusions:

  • Targeting PTEN offers therapeutic potential but faces significant hurdles.
  • Modulating PTEN's functional dose requires a comprehensive approach.
  • Future strategies should consider direct protein modulation, miRNA targeting, and gene/mRNA level interventions.
Keywords:
anti-geneanti-sensecancergene editingmiR-21miRNA maturationneurodegenerative diseasenew modalitiesphosphataseprotein-protein interaction

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