Chapter title |
Targeting AMPK: From Ancient Drugs to New Small-Molecule Activators.
|
---|---|
Chapter number | 13 |
Book title |
AMP-activated Protein Kinase
|
Published in |
EXS, November 2016
|
DOI | 10.1007/978-3-319-43589-3_13 |
Pubmed ID | |
Book ISBNs |
978-3-31-943587-9, 978-3-31-943589-3, 978-3-31-943587-9, 978-3-31-943589-3
|
Authors |
Bruno Guigas, Benoit Viollet, Guigas, Bruno, Viollet, Benoit |
Editors |
Mario D. Cordero, Benoit Viollet |
Abstract |
The AMP-activated protein kinase (AMPK) is an evolutionary conserved and ubiquitously expressed serine/threonine kinase mainly acting as a key regulator of cellular energy homeostasis. AMPK is a heterotrimeric protein complex, consisting of a catalytic α subunit and two regulatory β and γ subunits, whose activity is tightly regulated by changes in adenine nucleotides and several posttranslational modifications. Once activated in response to energy deficit, AMPK concomitantly inhibits ATP-consuming anabolic processes and promotes ATP-generating catabolic pathways via direct phosphorylation of multiple downstream effectors, leading to restoration of cellular energy balance. A growing number of energy/nutrient-independent functions of AMPK are also regularly reported, progressively expanding its role to regulation of non-metabolic cellular processes. Historically, AMPK as a therapeutic target has attracted much of interest due to its potential impact on metabolic disorders, such as obesity and type 2 diabetes, but has also recently received considerable renewed attention in the framework of cancer studies, highlighting the persistent need for selective, reversible, potent, and tissue-specific activators. In this chapter, we review the most recent advances in the understanding of the mechanism(s) of action of the current portfolio of AMPK activators, including plant-derived natural compounds and newly discovered small-molecule agonists directly targeting various AMPK subunits. |
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Members of the public | 1 | 100% |
Mendeley readers
Geographical breakdown
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Unknown | 38 | 100% |
Demographic breakdown
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Student > Master | 7 | 18% |
Student > Bachelor | 6 | 16% |
Researcher | 4 | 11% |
Professor | 2 | 5% |
Other | 2 | 5% |
Other | 6 | 16% |
Unknown | 11 | 29% |
Readers by discipline | Count | As % |
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Biochemistry, Genetics and Molecular Biology | 11 | 29% |
Medicine and Dentistry | 6 | 16% |
Agricultural and Biological Sciences | 4 | 11% |
Business, Management and Accounting | 1 | 3% |
Nursing and Health Professions | 1 | 3% |
Other | 4 | 11% |
Unknown | 11 | 29% |