| 李淑敏,李燕京,白玉贤.M2型丙酮酸激酶的抗肿瘤作用研究进展[J].中国肿瘤,2019,28(3):202-207. |
| M2型丙酮酸激酶的抗肿瘤作用研究进展 |
| Research Progress on Anticancer Effects of Pyruvate Kinase M2 |
| 投稿时间：2018-09-28 |
| DOI：10.11735/j.issn.1004-0242.2019.03.A008 |
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| 中文关键词: M2型丙酮酸激酶 Warburg效应 核转位 细胞增殖 激活剂 抑制剂 肿瘤代谢 |
| 英文关键词:pyruvate kinase M2 Warburg effect nuclear translocation cell proliferation activator inhibitor tumor metabolism |
| 基金项目:国家自然科学基金（青年项目，81602662）；吴阶平基金 (320.6750.16002)；哈尔滨医科大学附属肿瘤医院科学研究基金(BJQN2018-02，JJZ2011-18，JJMS2014-03) |
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| 中文摘要: |
| 摘 要：糖酵解（Warburg效应）是肿瘤细胞的重要特征，其相比于线粒体氧化磷酸化来说更高效地产生能量及大量的中间产物用于生物合成，还可抑制活性氧的生成。M2型丙酮酸激酶（pyruvate kinase M2，PKM2）多以低活性的二聚体形式存在于肿瘤细胞等快速增殖细胞中，作为催化糖酵解最后一个步骤的限速酶，是肿瘤细胞Warburg效应的一个关键调节因子。PKM2在肿瘤细胞中也发挥着重要的非代谢作用。PKM2被诱导转移入细胞核后，通过磷酸化特定的核蛋白后激活诸多基因的转录，促进肿瘤的生长。基于这些研究成果，该文综述了PKM2在肿瘤生长中的作用，并对PKM2的抑制剂和激活剂的抗肿瘤疗效分别进行讨论，并预测PKM2可能成为癌症治疗的潜在靶点。 |
| 英文摘要: |
| Abstract：Glycolysis(Warburg effect) is an important metabolic feature of tumor cells. Compared with mitochondrial oxidative phosphorylation，glycolysis promotes rapid energy production and a great number of glycolytic intermediates for biosynthesis without the accumulation of reactive oxygen species. Pyruvate kinase M2(PKM2) is expressed in proliferative cells and cancer cells. The predominant form of PKM2 is the dimer with lower activity. It is the rate-limiting enzyme of the last step of glycolysis and the critical regulatory factor of aerobic glycolysis. PKM2 also plays an important role in non-glycolytic functions. After translocating to nucleus，PKM2 phosphorylates specific nucleoproteins and activates the transcription of related genes to promote tumor growth. This article reviews the role of PKM2 in tumor cell growth，the anticancer effects of PKM2 activators and inhibitors，and explores the possibility of PKM2 as a potential target for cancer treatment. |
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