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

An update on therapeutic opportunities offered by cancer glycolytic metabolism.

Author information

1
Dipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
2
Drug Discovery Program, Experimental Oncology Department, European Institute of Oncology IEO, Via Adamello 16, 20139 Milan, Italy.
3
Dipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy. Electronic address: filippo.minutolo@farm.unipi.it.

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

PMID:
25288186
DOI:
10.1016/j.bmcl.2014.09.041
[Indexed for MEDLINE]
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