Identification of Akt-selective cytotoxic compounds that enhance cytotoxic responses to rapamycin

Cancer Biol Ther. 2010 Dec 15;10(12):1256-61. doi: 10.4161/cbt.10.12.13442. Epub 2010 Dec 15.

Abstract

We performed a high-throughput screen to identify compounds with a selective ability to induce apoptosis in Akt-expressing cells without disrupting Bcl-xL-dependent survival. Results showed that a screening strategy based on Alamar Blue underrepresented the viability of Bcl-xL-expressing cells relative to Akt-expressing cells, possibly due to metabolic differences between the two cell survival programs. Using an alternative screen based on plasma membrane integrity, we identified several compounds that target Akt-dependent survival without toxic effect to Bcl-xL-dependent survival. These compounds enhanced the cytotoxic potential of rapamycin, a chemotherapeutic that inhibits survival signaling downstream of Akt. The results demonstrate a screening method and the subsequent identification of two compounds with selective activity in counteracting Akt-dependent cell survival.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Caspase 3 / metabolism
  • Cell Line
  • Cell Membrane / drug effects
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Drug Discovery
  • Drug Screening Assays, Antitumor / methods
  • High-Throughput Screening Assays*
  • Mice
  • Oxazines
  • Phosphatidylinositol 3-Kinases / metabolism
  • Proto-Oncogene Proteins c-akt / antagonists & inhibitors
  • Proto-Oncogene Proteins c-akt / metabolism*
  • Signal Transduction / drug effects
  • Sirolimus / pharmacology*
  • Xanthenes
  • bcl-X Protein / genetics
  • bcl-X Protein / metabolism*

Substances

  • Antineoplastic Agents
  • Oxazines
  • Xanthenes
  • bcl-X Protein
  • resazurin
  • Phosphatidylinositol 3-Kinases
  • Proto-Oncogene Proteins c-akt
  • Caspase 3
  • Sirolimus