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

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• 作者：Kimberly O. Cameron^a ; ^{kimberly.o.cameron@pfizer.com" class="auth_mail" title="E-mail the corresponding author} ; Ravi G. Kurumbail^b
• 关键词：ACC ; acetyl-CoA carboxylase ; ADaM ; allosteric drug and metabolite ; AID ; auto-inhibitory domain ; α-RIM ; α-regulatory interacting motif ; AMPK ; adenosine monophosphate-activated protein kinase ; ASMS ; affinity selection mass spectrometry ; CamKKβ ; Ca2+/calmodulin-dependent protein kinase kinase-beta ; CBM ; carbohydrate binding module ; CBS ; cystathionine-β-synthase ; DNL ; de novo lipogenesis ; GLUT4 ; glucose transporter type 4 ; HDAC ; histone deacetylase ; HMG-CoA reductase ; 3-hydroxy-3-methyl-glutaryl-coe
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 November 2016
• 年：2016
• 卷：26
• 期：21
• 页码：5139-5148
• 全文大小：3789 K

文摘

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.