Cited by 387Metabolism, Diabetes, and CancerBiochemical and Molecular ResearchPeroxisome Proliferator-Activated Receptors

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AMPK inhibition in health and disease

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Viollet, Benoit, Horman, Sandrine, Leclerc, Jocelyne, Lantier, Louise, Foretz, Marc, Billaud, Marc, Giri, Shailendra, Andreelli, Fabrizio·2010·Critical Reviews in Biochemistry and Molecular Biology

DOI 10.3109/10409238.2010.488215PMC PMC3132561

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Abstract

All living organisms depend on dynamic mechanisms that repeatedly reassess the status of amassed energy, in order to adapt energy supply to demand. The AMP-activated protein kinase (AMPK) alphabetagamma heterotrimer has emerged as an important integrator of signals managing energy balance. Control of AMPK activity involves allosteric AMP and ATP regulation, auto-inhibitory features and phosphorylation of its catalytic (alpha) and regulatory (beta and gamma) subunits. AMPK has a prominent role not only as a peripheral sensor but also in the central nervous system as a multifunctional metabolic regulator. AMPK represents an ideal second messenger for reporting cellular energy state. For this reason, activated AMPK acts as a protective response to energy stress in numerous systems. However, AMPK inhibition also actively participates in the control of whole body energy homeostasis. In this review, we discuss recent findings that support the role and function of AMPK inhibition under physiological and pathological states.

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5 retracted

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BindingDB Entry 50013294: Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors.
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BindingDB Entry 50032478: The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity.
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BindingDB Entry 50006602: Pharmacological Targeting of AMP-Activated Protein Kinase and Opportunities for Computer-Aided Drug Design.
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Authors: Viollet, B., Horman, S., Leclerc, J., Lantier, L., Foretz, M., Billaud, M., Giri, S., & Andreelli, F.
Affiliations: UCLouvain (BE)
Inserm (FR)
Centre National de la Recherche Scientifique (FR)
Mayo Clinic (US)
ORCID: Horman, Sandrine
Lantier, Louise
Foretz, Marc
Billaud, Marc
Giri, Shailendra
Venue: Critical Reviews in Biochemistry and Molecular Biology
Publisher: Informa UK Limited
Published: 2010-06-04
Volume: 45
Issue: 4
Pages: 276-295
ISSN: 0045-6411 (ISSN-L)
1040-9238
1549-7798
DOI: 10.3109/10409238.2010.488215
PMC: PMC3132561
OpenAlex: W2015171350
Cited by: 383
References: 226
Citations by year: 2026: 14 · 2025: 15 · 2024: 11 · 2023: 18 · 2022: 22 · 2021: 23 · 2020: 39 · 2019: 22 · 2018: 34 · 2017: 33 · 2016: 38 · 2015: 30 · 2014: 27 · 2013: 25 · 2012: 19
FWCI: 1.62
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Locations: Critical Reviews in Biochemistry and Molecular Biology (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
HAL (submittedVersion, other-oa)
Digital Access to Libraries (Université catholique de Louvain (UCL), l'Université de Namur (UNamur) and the Université Saint-Louis (USL-B)) (submittedVersion, other-oa)
Digital Access to Libraries (Université catholique de Louvain (UCL), l'Université de Namur (UNamur) and the Université Saint-Louis (USL-B)) (submittedVersion)
Funders: European Commission
Agence Nationale de la Recherche (ANR-06-PHYS-0026)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Biochemical and Molecular Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Peroxisome Proliferator-Activated Receptors
Keywords: AMPK, AMPK inhibition, energy homeostasis, allosteric regulation, protein phosphorylation, central nervous system metabolism
MeSH terms: Animals, Energy Metabolism, Enzyme Activation, Humans, Down-Regulation, AMP-Activated Protein Kinases

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