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Drug discovery approaches targeting the PI3K/Akt pathway in cancer

C Garcia-Echeverria1, W R Sellers

  • 1Oncology Drug Discovery, Novartis Institutes for Biomedical Research, Basel, Switzerland. carlos.garcia-echeverria@novartis.com

Oncogene
|September 17, 2008
PubMed

Insights

The phosphatidylinositol 3-kinase (PI3K)/Akt pathway is crucial in human tumors. This review covers preclinical knowledge of PI3K/Akt pathway modulators, including clinical stage inhibitors and tool compounds.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The PI3K/Akt pathway is frequently activated in human cancers.
  • Genetic alterations like PTEN inactivation and PIK3CA mutations drive pathway activation.
  • This pathway is a key target for anticancer drug development.

Purpose of the Study:

  • To review preclinical knowledge of PI3K/Akt pathway modulators.
  • To focus on drug discovery and development activities.
  • To highlight clinical stage inhibitors and tool compounds.

Main Methods:

  • Literature review of preclinical studies.
  • Analysis of drug discovery and development data.
  • Focus on inhibitors targeting PI3K, PDK1, Akt, and HSP90.

Main Results:

  • Numerous PI3K/Akt pathway modulators are under investigation.
  • Clinical trials are ongoing for inhibitors of PI3K, Akt, and HSP90.
  • Preclinical data supports the development of targeted therapies.

Conclusions:

  • The PI3K/Akt pathway remains a significant target for cancer therapy.
  • Continued research into pathway modulators is essential for advancing cancer treatment.
  • Development of specific inhibitors shows promise for clinical application.

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