An update on therapeutic opportunities offered by cancer glycolytic metabolism

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:24

Article

Granchi, Carlotta¹  Fancelli, Daniele²  Minutolo, Filippo¹ 

[1] Univ Pisa, Dipartimento Farm, I-56126 Pisa, Italy

[2] European Inst Oncol IEO, Dept Expt Oncol, Drug Discovery Program, I-20139 Milan, Italy

关键词: Cancer metabolism;    Warburg effect;    Glycolysis;    Hypoxia;    Antitumor agents;   

DOI  :  10.1016/j.bmcl.2014.09.041

来源: Elsevier

【 摘 要 】

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. (C) 2014 The Authors. Published by Elsevier Ltd.

【 授权许可】

Free