Dual targeting of the Warburg effect with a glucose-conjugated lactate dehydrogenase inhibitor

Chembiochem. 2013 Nov 25;14(17):2263-7. doi: 10.1002/cbic.201300562. Epub 2013 Oct 31.

Abstract

Effective glucose diet: We report the development and activity of glucose-conjugated LDH-A inhibitors designed for dual targeting of the Warburg effect (elevated glucose uptake and glycolysis) in cancer cells. Glycoconjugation could be applied to inhibitors of many enzymes involved in glycolysis or tumor metabolism.

Keywords: Warburg effect; cancer; drug design; glycoconjugation; targeted anticancer agents.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Glucose / chemistry*
  • Glucose / metabolism
  • Glycolysis / drug effects
  • Humans
  • L-Lactate Dehydrogenase / antagonists & inhibitors*
  • L-Lactate Dehydrogenase / metabolism
  • Models, Molecular
  • Molecular Structure
  • Neoplasms / diagnosis
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Neoplasms / metabolism*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • L-Lactate Dehydrogenase
  • Glucose