AMPK activators: mechanisms of action and physiological activities.

AMPK activators: mechanisms of action and physiological activities.
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DOI:
10.1038/emm.2016.16
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发表时间:
2016-04-01
影响因子:
12.8
通讯作者:
Ha J
Ha J
中科院分区:
医学2区
文献类型:
--
作者:
Kim J;Yang G;Kim Y;Kim J;Ha J

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amp活化蛋白激酶(AMPK)是能量稳态的中心调节器,它协调代谢途径,从而平衡营养供应和能量需求。由于AMPK活化对代谢具有良好的生理效果,AMPK已被认为是控制代谢综合征和癌症等人类疾病的重要治疗靶点。因此,AMPK的激活剂可能有潜力作为这些疾病的新疗法。在这篇综述中,我们全面总结了间接和直接AMPK激活剂及其与AMPK结构相关的作用模式。我们讨论了异构体特异性AMPK复合物之间的功能差异,以及它们在开发新型AMPK激活剂方面的意义,以及结合不同AMPK激活剂治疗人类疾病的潜力。
AMP-activated protein kinase (AMPK) is a central regulator of energy homeostasis, which coordinates metabolic pathways and thus balances nutrient supply with energy demand. Because of the favorable physiological outcomes of AMPK activation on metabolism, AMPK has been considered to be an important therapeutic target for controlling human diseases including metabolic syndrome and cancer. Thus, activators of AMPK may have potential as novel therapeutics for these diseases. In this review, we provide a comprehensive summary of both indirect and direct AMPK activators and their modes of action in relation to the structure of AMPK. We discuss the functional differences among isoform-specific AMPK complexes and their significance regarding the development of novel AMPK activators and the potential for combining different AMPK activators in the treatment of human disease.