Suppression of tumor energy supply by liposomal nanoparticle-mediated inhibition of aerobic glycolysis

Yinlong Zhang, Jingyan Wei, Jiaqi Xu, Wei Sun Leong, Guangna Liu, Tianjiao Ji, Zhiqiang Cheng, Jing Wang, Jiayan Lang, Ying Zhao, Linhao You, Xiao Zhao, Taotao Wei, Greg J. Anderson, Sheng Qi, Jing Kong, Guangjun Nie, Suping Li

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Aerobic glycolysis enables cancer cells to rapidly take up nutrients (e.g., nucleotides, amino acids, and lipids) and incorporate them into the biomass needed to produce a new cell. In contrast to existing chemotherapy/radiotherapy strategies, inhibiting aerobic glycolysis to limit the adenosine 5′-triphosphate (ATP) yield is a highly efficient approach for suppressing tumor cell proliferation. However, most, if not all, current inhibitors of aerobic glycolysis cause significant adverse effects because of their nonspecific delivery and distribution to nondiseased organs, low bioavailability, and a narrow therapeutic window. New strategies to enhance the biosafety and efficacy of these inhibitors are needed for moving them into clinical applications. To address this need, we developed a liposomal nanocarrier functionalized with a well-validated tumor-targeting peptide to specifically deliver the aerobic glycolysis inhibitor 3-bromopyruvate (3-BP) into the tumor tissue. The nanoparticles effectively targeted tumors after systemic administration into tumor-bearing mice and suppressed tumor growth by locally releasing 3-BP to inhibit the ATP production of the tumor cells. No overt side effects were observed in the major organs. This report demonstrates the potential utility of the nanoparticle-enabled delivery of an aerobic glycolysis inhibitor as an anticancer therapeutic agent.
Original languageEnglish
Pages (from-to)2347–2353
Number of pages7
JournalACS Applied Materials & Interfaces
Issue number3
Early online date29 Dec 2017
Publication statusPublished - 24 Jan 2018


  • 3-bromopyruvate
  • ATP
  • liposomal nanoparticles
  • tumor-targeting peptide
  • Warburg effect

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