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

Zhang, Yinlong, Wei, Jingyan, Xu, Jiaqi, Leong, Wei Sun, Liu, Guangna, Ji, Tianjiao, Cheng, Zhiqiang, Wang, Jing, Lang, Jiayan, Zhao, Ying, You, Linhao, Zhao, Xiao, Wei, Taotao, Anderson, Greg J., Qi, Sheng ORCID:, Kong, Jing, Nie, Guangjun and Li, Suping (2018) Suppression of tumor energy supply by liposomal nanoparticle-mediated inhibition of aerobic glycolysis. ACS Applied Materials & Interfaces, 10 (3). 2347–2353. ISSN 1944-8244

[thumbnail of revised and accepted manuscript]
PDF (revised and accepted manuscript) - Accepted Version
Download (1MB) | Preview


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.

Item Type: Article
Uncontrolled Keywords: 3-bromopyruvate,atp,liposomal nanoparticles,tumor-targeting peptide,warburg effect,sdg 3 - good health and well-being ,/dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being
Faculty \ School: Faculty of Science > School of Pharmacy
UEA Research Groups: Faculty of Science > Research Groups > Pharmaceutical Materials and Soft Matter
Related URLs:
Depositing User: LivePure Connector
Date Deposited: 20 Jul 2018 15:32
Last Modified: 21 Oct 2022 19:30
DOI: 10.1021/acsami.7b16685


Downloads per month over past year

Actions (login required)

View Item View Item