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Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
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PTEN modulators: a patent review

Chandra S Boosani1, Devendra K Agrawal

  • 1Creighton University School of Medicine, Department of Biomedical Sciences, Omaha, NE 68178, USA.

Expert Opinion on Therapeutic Patents
|February 6, 2013
PubMed
Abstract

Insights

Phosphatase and tensin homolog (PTEN) regulates cell signaling and survival; its inactivation by phosphorylation is linked to diseases. Targeting kinases affecting PTEN offers therapeutic potential for various PTEN-related conditions.

Area of Science:

  • Molecular Biology
  • Cell Signaling
  • Oncology

Background:

  • PTEN (phosphatase and tensin homolog deleted on chromosome 10) is a critical regulator of the PI3K/Akt pathway, controlling cell survival and proliferation.
  • PTEN dysfunction and mutations are implicated in numerous neoplastic and pathological conditions.
  • PTEN is inactivated by phosphorylation, unlike many proteins activated by this process.

Purpose of the Study:

  • To review the clinical relevance of PTEN modulators.
  • To identify novel molecular targets for drug development in PTEN-related diseases.
  • To explore therapeutic strategies for conditions including cardiovascular diseases, diabetes, obesity, cancer, autism, Parkinson's, and Alzheimer's.

Main Methods:

  • Comprehensive literature review of PTEN function and regulation.
  • Analysis of identified PTEN modulators and their clinical significance.
  • Proposal of novel molecular targets based on PTEN's role in disease.

Main Results:

  • PTEN's role in cell signaling is crucial, with its inactivation by phosphorylation being a key mechanism in disease.
  • Numerous PTEN modulators have been identified, highlighting its complex regulatory network.
  • Specific C-terminal phosphorylation sites in PTEN are critical for its inactivation.

Conclusions:

  • Targeting kinases that phosphorylate PTEN presents a promising therapeutic avenue.
  • Restoring normal PTEN function through novel drug candidates is essential for treating diverse human diseases.
  • The identified target sites offer potential for developing drugs to manage PTEN-related pathologies.

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