An update on therapeutic opportunities offered by cancer glycolytic metabolism

Bioorg Med Chem Lett. 2014 Nov 1;24(21):4915-25. doi: 10.1016/j.bmcl.2014.09.041. Epub 2014 Sep 20.

Abstract

Almost all invasive cancers, regardless of tissue origin, are characterized by specific modifications of their cellular energy metabolism. In fact, a strong predominance of aerobic glycolysis over oxidative phosphorylation (Warburg effect) is usually associated with aggressive tumour phenotypes. This metabolic shift offers a survival advantage to cancer cells, since they may continue to produce energy and anabolites even when they are exposed to either transient or permanent hypoxic conditions. Moreover, it ensures a high production rate of glycolysis intermediates, useful as building blocks for fast cell proliferation of cancer cells. This peculiar metabolic profile may constitute an ideal target for therapeutic interventions that selectively hit cancer cells with minimal residual systemic toxicity. In this review we provide an update about some of the most recent advances in the discovery of new bioactive molecules that are able to interfere with cancer glycolysis.

Keywords: Antitumor agents; Cancer metabolism; Glycolysis; Hypoxia; Warburg effect.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Glycolysis / drug effects*
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism*

Substances

  • Antineoplastic Agents