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Lapachol inhibits glycolysis in cancer cells by targeting pyruvate kinase M2

Mani Shankar Babu1, Sailendra Mahanta2, Alexander J Lakhter1

  • 1Department of Microbiology and Immunology, Indiana University School of Medicine, Indianapolis, Indiana, United States of America.

Plos One
|February 3, 2018
PubMed

Insights

Lapachol inhibits pyruvate kinase M2 (PKM2), a key enzyme in cancer glycolysis. This finding offers a new strategy for cancer therapy by targeting tumor cell metabolism.

Area of Science:

  • Biochemistry
  • Oncology
  • Molecular Biology

Background:

  • Aerobic glycolysis is a hallmark of cancer.
  • Pyruvate kinase M2 (PKM2) is crucial for cancer cell glycolysis.
  • Targeting PKM2 for cancer therapy is challenging due to a lack of selective agents.

Purpose of the Study:

  • To investigate lapachol as a potential inhibitor of PKM2.
  • To explore the effects of lapachol on melanoma cell metabolism and proliferation.
  • To assess lapachol's potential in cancer therapeutic strategies.

Main Methods:

  • In silico docking studies to identify lapachol binding to PKM2.
  • Enzyme activity assays using purified PKM2 and melanoma cell extracts.
  • Measurement of glycolysis, oxygen consumption, and ATP levels in lapachol-treated melanoma cells.
  • Assessment of cell proliferation and apoptosis induction.

Main Results:

  • Lapachol demonstrated high affinity binding to PKM2.
  • Lapachol inhibited PKM2 activity in vitro and in cell extracts.
  • Lapachol treatment reduced glycolysis, decreased ATP levels, and inhibited melanoma cell proliferation.
  • Lapachol sensitized cells to apoptosis induction.

Conclusions:

  • Lapachol acts as a PKM2 inhibitor, impacting cancer cell metabolism.
  • Lapachol represents a potential therapeutic agent for targeting tumor glycolysis.
  • Further research into lapachol's mechanism and efficacy is warranted for cancer treatment.

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