ArticleNutrients2023
Ellagic Acid and Its Metabolites as Potent and Selective Allosteric Inhibitors of Liver Pyruvate Kinase.
Article in Nutrients, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Symmetry-guided fusion converts weak liver pyruvate kinase inhibitors into potent allosteric activators.RSC medicinal chemistry · 2026Article
- Ellagic Acid Reduces Inulin's Adverse Effects: A Combined Approach to Enhance Therapeutic Potential in Nonalcoholic Steatohepatitis.Molecular nutrition & food research · 2026Article
- Genome-scale models in human metabologenomics.Nature reviews. Genetics · 2025Review
- Control of Neonatal Diarrhea in Piglets with Reduced Antibiotic Use by Application of a Complementary Feed-A Randomized Controlled Farm Trial.Veterinary sciences · 2025Article
- Role of pyruvate kinase M2 in regulating sepsis (Review).Molecular medicine reports · 2024Review
- Discovery of Cell-Permeable Allosteric Inhibitors of Liver Pyruvate Kinase: Design and Synthesis of Sulfone-Based Urolithins.International journal of molecular sciences · 2024Article
- Exploration of Novel Urolithin C Derivatives as Non-Competitive Inhibitors of Liver Pyruvate Kinase.Pharmaceuticals (Basel, Switzerland) · 2023Article
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Authors and funding
21 authors.
Funding
Abstract
Liver pyruvate kinase (PKL) has recently emerged as a new target for non-alcoholic fatty liver disease (NAFLD), and inhibitors of this enzyme could represent a new therapeutic option. However, this breakthrough is complicated by selectivity issues since pyruvate kinase exists in four different isoforms. In this work, we report that ellagic acid (EA) and its derivatives, present in numerous fruits and vegetables, can inhibit PKL potently and selectively. Several polyphenolic analogues of EA were synthesized and tested to identify the chemical features responsible for the desired activity. Molecular modelling studies suggested that this inhibition is related to the stabilization of the PKL inactive state. This unique inhibition mechanism could potentially herald the development of new therapeutics for NAFLD.
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