Structure and Physiological Regulation of AMPK

doi:10.3390/ijms19113534

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物靶标结构与功能中心

	Structure and Physiological Regulation of AMPK
	Yan, Yan 1,2; Zhou, X. Edward 2; Xu, H. Eric1,2 ; Melcher, Karsten 2
刊名	INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
	2018-11
卷号	19 期号:11
关键词	energy metabolism AMPK activation loop AID -linker -linker CBS LKB1 CaMKK2 RIM
ISSN号	1422-0067
DOI	10.3390/ijms19113534
文献子类	Review
英文摘要	Adenosine monophosphate (AMP)-activated protein kinase (AMPK) is a heterotrimeric complex that functions as a central regulator of energy homeostasis. Energy stress manifests as a drop in the ratio of adenosine triphosphate (ATP) to AMP/ADP, which activates AMPK's kinase activity, allowing it to upregulate ATP-generating catabolic pathways and to reduce energy-consuming catabolic pathways and cellular programs. AMPK senses the cellular energy state by competitive binding of the three adenine nucleotides AMP, ADP, and ATP to three sites in its subunit, each, which in turn modulates the activity of AMPK's kinase domain in its subunit. Our current understanding of adenine nucleotide binding and the mechanisms by which differential adenine nucleotide occupancies activate or inhibit AMPK activity has been largely informed by crystal structures of AMPK in different activity states. Here we provide an overview of AMPK structures, and how these structures, in combination with biochemical, biophysical, and mutational analyses provide insights into the mechanisms of adenine nucleotide binding and AMPK activity modulation.
资助项目	Van Andel Research Institute[00000000] ; National Institutes of Health[R01 GM129436]
WOS关键词	ACTIVATED PROTEIN-KINASE ; ENERGY SENSOR ; PHOSPHORYLATION ; MECHANISM ; SUBUNIT ; BINDING ; ALPHA ; UPSTREAM ; DOMAIN ; DRUGS
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
语种	英语
出版者	MDPI
WOS记录号	WOS:000451528500250
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279503]
专题	药物靶标结构与功能中心
通讯作者	Melcher, Karsten
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, VARI SIMM Ctr,Ctr Struct & Funct Drug Targets, Shanghai 201203, Peoples R China 2.Van Andel Res Inst, Ctr Canc & Cell Biol, 333 Bostwick Ave NE, Grand Rapids, MI 49503 USA;
推荐引用方式 GB/T 7714	Yan, Yan,Zhou, X. Edward,Xu, H. Eric,et al. Structure and Physiological Regulation of AMPK[J]. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES,2018,19(11).
APA	Yan, Yan,Zhou, X. Edward,Xu, H. Eric,&Melcher, Karsten.(2018).Structure and Physiological Regulation of AMPK.INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES,19(11).
MLA	Yan, Yan,et al."Structure and Physiological Regulation of AMPK".INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES 19.11(2018).