ArticleNature communications2016
Structural basis of allosteric and synergistic activation of AMPK by furan-2-phosphonic derivative C2 binding.
Article in Nature communications, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers, 1 of them a synthesis that pooled it.
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Who cites it
42 citing papers in PubMed, 1 synthesis or guideline pooled it, 87 citations in OpenAlex.
- AICAr, a Widely Used AMPK Activator with Important AMPK-Independent Effects: A Systematic Review.Cells · 2021Pooled it
- A phosphorylation switch at MRE11 links ATM-ATR and calcium signaling to safeguard stalled replication fork stability.Research square · 2026Article
- Discovering anti-obesity blue food compounds via combined deep learning and in silico approaches.Molecular diversity · 2026Article
- Transcriptional control of PPP2CB by YAP1 and TEAD1 mediates AMPK inhibition and mTORC1 activation in vascular smooth muscle cells.iScience · 2026Article
- Mechanism and cellular actions of the potent AMPK inhibitor BAY-3827.Science advances · 2025Article
- Small Molecule Modulators of AMP-Activated Protein Kinase (AMPK) Activity and Their Potential in Cancer Therapy.Journal of medicinal chemistry · 2025Review
- In silico design and computational screening of berberine derivatives for potential antidiabetic activity through allosteric activation of the AMPK pathway.In silico pharmacology · 2025Article
- AMPK phosphosite profiling by label-free mass spectrometry reveals a multitude of mTORC1-regulated substrates.npj metabolic health and disease · 2025Article
- The metabolic sensor AMPK: Twelve enzymes in one.Molecular metabolism · 2024Review
- The pro-drug C13 activates AMPK by two distinct mechanisms.The Biochemical journal · 2024Article
- Review
- Structure-function analysis of the AMPK activator SC4 and identification of a potent pan AMPK activator.The Biochemical journal · 2022Article
- The glucotoxicity protecting effect of honokiol in human hepatocytesFrontiers in nutrition · 2022Article
- Adenosine monophosphate activated protein kinase contributes to skeletal muscle health through the control of mitochondrial function.Frontiers in pharmacology · 2022Review
- Compound- and fiber type-selective requirement of AMPKγ3 for insulin-independent glucose uptake in skeletal muscle.Molecular metabolism · 2021Article
- Post-Translational Modifications of the Energy Guardian AMP-Activated Protein Kinase.International journal of molecular sciences · 2021Review
- AMP-Activated Protein Kinase: Do We Need Activators or Inhibitors to Treat or Prevent Cancer?International journal of molecular sciences · 2020Review
- Long-chain fatty acyl-CoA esters regulate metabolism via allosteric control of AMPK β1 isoforms.Nature metabolism · 2020Article
- ADP is the dominant controller of AMP-activated protein kinase activity dynamics in skeletal muscle during exercise.PLoS computational biology · 2020Article
- The AMP-Activated Protein Kinase Plays a Role in Antioxidant Defense and Regulation of Vascular Inflammation.Antioxidants (Basel, Switzerland) · 2020Review
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The metabolic stress-sensing enzyme AMP-activated protein kinase (AMPK) is responsible for regulating metabolism in response to energy supply and demand. Drugs that activate AMPK may be useful in the treatment of metabolic diseases including type 2 diabetes. We have determined the crystal structure of AMPK in complex with its activator 5-(5-hydroxyl-isoxazol-3-yl)-furan-2-phosphonic acid (C2), revealing two C2-binding sites in the γ-subunit distinct from nucleotide sites. C2 acts synergistically with the drug A769662 to activate AMPK α1-containing complexes independent of upstream kinases. Our results show that dual drug therapies could be effective AMPK-targeting strategies to treat metabolic diseases.
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