PI3K/Akt/mTOR inhibitors in cancer: At the bench and bedside

Ali S Alzahrani1

  • 1Division of Molecular Endocrinology, Department of Molecular Oncology, King Faisal Specialist Hospital and Research Centre, PO Box 3354, Research Center (MBC 03), Riyadh, 11211, Saudi Arabia.

Insights

The Phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) pathway is crucial for cell functions and often activated in cancer. Inhibiting this pathway with small molecules shows promise for targeted cancer therapy.

Area of Science:

  • Molecular Biology
  • Cellular Signaling
  • Oncology

Background:

  • The Phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) pathway is a critical regulator of fundamental cellular processes.
  • This pathway controls cell proliferation, growth, metabolism, and motility.
  • Aberrant activation of PI3K/Akt/mTOR pathway genes is frequently observed in human cancers.

Purpose of the Study:

  • To review recent advancements in targeting the PI3K/Akt/mTOR pathway for cancer treatment.
  • To discuss the development and application of small molecule inhibitors in molecular targeted therapy.
  • To highlight FDA-approved inhibitors and ongoing clinical evaluations.

Main Methods:

  • Literature review of preclinical and clinical studies.
  • Analysis of small molecule inhibitors targeting the PI3K/Akt/mTOR pathway.
  • Examination of regulatory approvals and trial outcomes.

Main Results:

  • Inhibition of the PI3K/Akt/mTOR pathway has demonstrated tumor regression in preclinical models.
  • Numerous clinical trials have evaluated PI3K/Akt/mTOR inhibitors.
  • Several inhibitors have received FDA approval based on demonstrated efficacy and safety.

Conclusions:

  • Targeting the PI3K/Akt/mTOR pathway represents a significant strategy in molecular cancer therapy.
  • Small molecule inhibitors are effective tools for this targeted approach.
  • Continued research and clinical trials are essential for optimizing PI3K/Akt/mTOR-based cancer treatments.

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