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Drugging ACAT1 for Cancer Therapy

Javier Garcia-Bermudez1, Kivanç Birsoy1

  • 1Laboratory of Metabolic Regulation and Genetics, The Rockefeller University, 1230 York Avenue, New York, NY 10065, USA.

Molecular Cell
|December 3, 2016
PubMed

Insights

Oncogenic tyrosine kinases promote cancer glycolysis by stabilizing mitochondrial acetyl-CoA acetyltransferase 1 (ACAT1). A novel ACAT1 inhibitor shows promising anti-cancer effects.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Mitochondrial acetyl-CoA acetyltransferase 1 (ACAT1) plays a role in cellular metabolism.
  • Aberrant glycolysis is a hallmark of cancer cells, often driven by oncogenic signaling pathways.

Purpose of the Study:

  • To investigate the role of oncogenic tyrosine kinases in regulating ACAT1.
  • To explore the potential of targeting ACAT1 for anti-cancer therapy.

Main Methods:

  • Phosphorylation assays to determine ACAT1 stabilization by tyrosine kinases.
  • Glycolysis measurements in cancer cells.
  • Screening for small molecule inhibitors of ACAT1.
  • In vitro and in vivo anti-cancer efficacy studies.

Main Results:

  • Oncogenic tyrosine kinases phosphorylate and stabilize the tetrameric form of ACAT1.
  • ACAT1 stabilization by kinases enhances glycolysis in cancer cells.
  • A novel small molecule inhibitor of ACAT1 was identified.
  • This ACAT1 inhibitor demonstrated significant anti-cancer effects.

Conclusions:

  • Oncogenic tyrosine kinases promote cancer cell glycolysis through ACAT1 stabilization.
  • Targeting ACAT1 with small molecule inhibitors represents a potential therapeutic strategy for cancer treatment.

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