The sweet trap in tumors: aerobic glycolysis and potential targets for therapy

Li Yu _, Xun Chen, Liantang Wang and Shangwu Chen

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Oncotarget. 2016; 7:38908-38926. https://doi.org/10.18632/oncotarget.7676

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Li Yu1,*, Xun Chen2,*, Liantang Wang1 and Shangwu Chen3

1 Department of Pathology, The First Affiliated Hospital, Sun Yat-sen (Zhongshan) University, Guangzhou, P.R. China

2 Guanghua School of Stomatology, Hospital of Stomatology, Sun Yat-sen University, Guangzhou, P.R. China

3 State Key Laboratory for Biocontrol, Guangdong Key Laboratory of Pharmaceutical Functional Genes, Department of Biochemistry, School of Life Sciences, Sun Yat-sen (Zhongshan) University, Guangzhou, P.R. China

* These authors have contributed equally to this work

Correspondence to:

Li Yu, email:

Shangwu Chen, email:

Keywords: aerobic glycolysis; Warburg effect; glucose metabolism; targets for the tumor therapy

Received: November 04, 2015 Accepted: February 16, 2016 Published: February 24, 2016


Metabolic change is one of the hallmarks of tumor, which has recently attracted a great of attention. One of main metabolic characteristics of tumor cells is the high level of glycolysis even in the presence of oxygen, known as aerobic glycolysis or the Warburg effect. The energy production is much less in glycolysis pathway than that in tricarboxylic acid cycle. The molecular mechanism of a high glycolytic flux in tumor cells remains unclear. A large amount of intermediates derived from glycolytic pathway could meet the biosynthetic requirements of the proliferating cells. Hypoxia-induced HIF-1α, PI3K-Akt-mTOR signaling pathway, and many other factors, such as oncogene activation and tumor suppressor inactivation, drive cancer cells to favor glycolysis over mitochondrial oxidation. Several small molecules targeting glycolytic pathway exhibit promising anticancer activity both in vitro and in vivo. In this review, we will focus on the latest progress in the regulation of aerobic glycolysis and discuss the potential targets for the tumor therapy.

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