Novikova D S, Garabadzhiu A V, Melino G, Barlev N A, Tribulovich V G
Saint Petersburg State Technological Institute (Technical University), St. Petersburg, 190013, Russia.
Biochemistry (Mosc). 2015 Feb;80(2):127-44. doi: 10.1134/S0006297915020017.
Recently, AMP-activated protein kinase (AMPK) has emerged as a key regulator of energy balance at cellular and whole-body levels. Due to the involvement in multiple signaling pathways, AMPK efficiently controls ATP-consuming/ATP-generating processes to maintain energy homeostasis under stress conditions. Loss of the kinase activity or attenuation of its expression leads to a variety of metabolic disorders and increases cancer risk. In this review, we discuss recent findings on the structure of AMPK, its activation mechanisms, as well as the consequences of its targets in regulation of metabolism. Particular attention is given to low-molecular-weight compounds that activate or inhibit AMPK; the perspective of therapeutic use of such modulators in treatment of several common diseases is discussed.
最近,AMP激活的蛋白激酶(AMPK)已成为细胞和全身水平能量平衡的关键调节因子。由于参与多种信号通路,AMPK在应激条件下能有效控制ATP消耗/ATP生成过程,以维持能量稳态。激酶活性丧失或其表达减弱会导致多种代谢紊乱,并增加癌症风险。在本综述中,我们讨论了关于AMPK结构、其激活机制以及其靶点在代谢调节中的作用的最新研究结果。特别关注激活或抑制AMPK的低分子量化合物;并讨论了此类调节剂在治疗几种常见疾病中的治疗应用前景。