期刊
JOURNAL OF BIOENERGETICS AND BIOMEMBRANES
卷 44, 期 1, 页码 7-15出版社
SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s10863-012-9419-2
关键词
3-bromopyruvate; Cancer; Energy metabolism; Chemotherapy; toxicity
资金
- Swedish Cancer Society
- Radiumhemmet Research Funds
- foundation Goljes Minne
- foundation Olle Engkvist Byggmastare
The pyruvate mimetic 3-bromopyruvate (3-BP) is generally presented as an inhibitor of glycolysis and has shown remarkable efficacy in not only preventing tumor growth, but even eradicating existant tumors in animal studies. We here review reported molecular targets of 3-BP and suggest that the very range of possible targets, which pertain to the altered energy metabolism of tumor cells, contributes both to the efficacy and the tumor specificity of the drug. Its in vivo efficacy is suggested to be due to a combination of glycolytic and mitochondrial targets, as well as to secondary effects affecting the tumor microenvironment. The cytotoxicity of 3-BP is less due to pyruvate mimicry than to alkylation of, e.g., key thiols. Alkylation of DNA/RNA has not been reported. More research is warranted to better understand the pharmacokinetics of 3-BP, and its potential toxic effects to normal cells, in particular those that are highly ATP-/mitochondrion-dependent.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据