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

Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators
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DOI:
10.1016/j.bmcl.2016.09.065
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发表时间:
2016-11-01
影响因子:
2.7
通讯作者:
Kurumbail, Ravi G.
Kurumbail, Ravi G.
中科院分区:
医学4区
文献类型:
--
作者:
Cameron, Kimberly O.;Kurumbail, Ravi G.

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腺苷一磷酸活化蛋白激酶(AMPK)是一种丝氨酸/苏氨酸异源三聚体蛋白激酶,是细胞和全身能量稳态的关键调节因子。有12种已知的AMPK同种型在组织和物种中差异表达。AMPK信号传导的失调与多种人类病理学相关。因此,AMPK的异构体选择性激活剂正在积极寻求用于治疗心血管和代谢疾病。本文综述了AMPK直接激活剂的专利和公开文献。(C)2016爱思唯尔有限公司版权所有
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.