基础医学与临床 ›› 2008, Vol. 28 ›› Issue (11): 1212-1215.

• 短篇综述 • 上一篇    下一篇

丙酮酸脱氢酶激酶的研究进展

菅记涌 张勇 朱大海   

  1. 中国医学科学院 北京协和医学院 基础医学研究所 中国医学科学院 北京协和医学院 基础医学研究所 中国医学科学院 北京协和医学院 基础医学研究所
  • 收稿日期:2008-07-10 修回日期:2008-08-11 出版日期:2008-11-25 发布日期:2008-11-25
  • 通讯作者: 朱大海

Research progresses on pyruvate dehydrogenase kinases

Ji-yong JIAN, Yong ZHANG, Da-hai ZHU   

  1. Institute of Basic Medical Science, CAMS & PUMC, Beijing 100005,China Institute of Basic Medical Science, CAMS & PUMC, Beijing 100005,China Institute of Basic Medical Science, CAMS & PUMC, Beijing 100005,China
  • Received:2008-07-10 Revised:2008-08-11 Online:2008-11-25 Published:2008-11-25
  • Contact: Da-hai ZHU

摘要: 丙酮酸脱氢酶激酶(PDK)具有能够调节线粒体丙酮酸脱氢酶复合体(PDC)催化丙酮酸脱羧氧化的活性,并进一步将糖酵解与三羧酸循环以及ATP的生成联系在一起。本综述主要介绍了PDKs的调节机制以及PDKs抑制剂在降低血糖、减少心肌缺血时造成的损伤和诱导肿瘤细胞凋亡中的作用。PDKs有可能成为糖尿病、心肌缺血和癌症治疗的潜在药物靶点。

关键词: 丙酮酸脱氢酶复合体, 丙酮酸脱氢酶激酶, 糖尿病, 心脏缺血, 癌症

Abstract: Pyruvate dehydrogenase kinases (PDKs 1-4) can regulate the activity of the mitochondrial pyruvate dehydrogenase complex (PDC) to catalyse the oxidative decarboxylation of pyruvate, and then links glycolysis to the tricarboxylic acid cycle and ATP production. In this review, we summarize recent significant advances in our knowledge of the mechanisms regulating PDKs and the function of PDKs inhibitors in lowering blood glucose, decreasing damage during heart ischemia and also triggering apoptosis in cancer cells. PDKs will be a possible pharmacological targets in diabetes,heart ischemia and cancer therapy.

Key words: pyruvate dehydrogenase complex, pyruvate dehydrogenase kinases, diabetes, heart ischemia, cancer