Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators

被引：37
|
作者：
Cameron, Kimberly O. [1 ]
Kurumbail, Ravi G. [2 ]
机构：
[1] Pfizer Global Res & Dev, Cardiovasc & Metab Dis Chem, 610 Main St, Cambridge, MA 02139 USA
[2] Pfizer Global Res & Dev, Worldwide Med Chem, Eastern Point Rd, Groton, CT 06340 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 21期
关键词：
AMPK; Enzyme activators; Crystallography; CBS; Allostery; CBM; MOUSE SKELETAL-MUSCLE; STRUCTURAL BASIS; ADIPOSE-TISSUE; GLUCOSE-UPTAKE; HETEROTRIMERIC COMPLEXES; MITOCHONDRIAL FISSION; INSULIN SENSITIVITY; METABOLIC SYNDROME; RESPIRATORY-CHAIN; GLYCOGEN-CONTENT;
D O I：
10.1016/j.bmcl.2016.09.065
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Adenosine monophosphate-activated protein kinase (AMPK), a serine/threonine heterotrimeric protein kinase, is a critical regulator of cellular and whole body energy homeostasis. There are twelve known AMPK isoforms that are differentially expressed in tissues and species. Dysregulation of AMPK signaling is associated with a multitude of human pathologies. Hence isoform-selective activators of AMPK are actively being sought for the treatment of cardiovascular and metabolic diseases. The present review summarizes the status of direct AMPK activators from the patent and published literature. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5139 / 5148
页数：10
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