Small Molecule Adenosine 5′-Monophosphate Activated Protein Kinase (AMPK) Modulators and Human Diseases

被引：56
|
作者：
Rana, Sandeep [1 ]
Blowers, Elizabeth C. [1 ]
Natarajan, Amarnath [1 ]
机构：
[1] Univ Nebraska Med Ctr, Eppley Inst Res Canc & Allied Dis, Omaha, NE 68198 USA
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2015年 / 58卷 / 01期
关键词：
ALPHA-LIPOIC ACID; ACETYL-COA CARBOXYLASE; STIMULATED GLUCOSE-UPTAKE; FLUORESCENCE POLARIZATION ASSAY; CANCER-CELL-PROLIFERATION; RESPIRATORY COMPLEX-I; LKB1; TUMOR-SUPPRESSOR; HUMAN SKELETAL-MUSCLE; GREEN TEA POLYPHENOL; ALZHEIMERS-DISEASE;
D O I：
10.1021/jm401994c
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Adenosine 5'-monophosphate activated protein kinase (AMPK) is a master sensor of cellular energy status that plays a key role in the regulation of whole-body energy homeostasis. AMPK is a serine/threonine kinase that is activated by upstream kinases LKB1, CaMKK beta, and Tak1, among others. AMPK exists as a beta? trimeric complexes that are allosterically regulated by AMP, ADP, and ATP. Dysregulation of AMPK has been implicated in a number of metabolic diseases including type 2 diabetes mellitus and obesity. Recent studies have associated roles of AMPK with the development of cancer and neurological disorders, making it a potential therapeutic target to treat human diseases. This review focuses on the structure and function of AMPK, its role in human diseases, and its direct substrates and provides a brief synopsis of key AMPK modulators and their relevance in human diseases.
引用
收藏
页码：2 / 29
页数：28
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