ArticleNature communications2024
Structural basis for urate recognition and apigenin inhibition of human GLUT9.
Article in Nature communications, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed.
- 6'‑O‑Caffeoylarbutin attenuates experimental hyperuricemia by regulating renal and intestinal urate transport, intestinal barrier integrity, and gut microbiota.Molecular medicine reports · 2026Article
- Substrate binding reorganizes the energetic landscape of Plasmodium falciparum hexose transporter PfHT1.bioRxiv : the preprint server for biology · 2026Article
- ABCG2 transporter: Structural and functional associations with gout (Review).International journal of molecular medicine · 2026Review
- Glucose Transporters: Structure, Trafficking, Physiology, and Disease Relevance.Current issues in molecular biology · 2026Review
- Blue Honeysuckle Extract Ameliorates Hyperuricemia by Modulating Gut Microbiota and Improving Liver-Kidney-Gut Axis Function.Antioxidants (Basel, Switzerland) · 2026Article
- Urate transporters: Structural mechanisms and therapeutic opportunities in drug development.Acta pharmaceutica Sinica. B · 2026Article
- Identification of Bruceine A as a novel HSP90AB1 inhibitor for suppressing hepatocellular carcinoma growth.Journal of advanced research · 2026Article
- A two-step mechanism for sugar translocation.Nature structural & molecular biology · 2026Article
- A Novel Dual URAT1/GLUT9 Inhibitor Reduces Hyperuricemia by Enhancing Uric Acid Excretion and Attenuating Renal Fibrosis.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Structure-Based Virtual Screening of Plant-Derived Flavonoids as Putative GLUT9 Binders with Antioxidant Properties.Molecules (Basel, Switzerland) · 2026Article
- Insulin Resistance and Inflammation.International journal of molecular sciences · 2026Review
- Overcoming the Low Bioavailability of Apigenin: The Therapeutic Efficacy for Androgenetic Alopecia Through Topical Administration.Food science & nutrition · 2025Article
- Molecular interplay between TXNIP and GLUT9 underlies uric acid transport dysregulation in vitro under hyperuricemic stress.European journal of medical research · 2025Article
- Association of SNPs in carbohydrate metabolism genes with insulin resistance indicators in the Mexican population.Nutrition & metabolism · 2025Article
- Structural Insights into the Substrate Egress Pathways Explains Specificity and Inhibition of Human Glucose Transporters (GLUT1 and GLUT9).ACS pharmacology & translational science · 2025Article
- Structural basis of disease mutation and substrate recognition by the human SLC2A9 transporter.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- In Slico Screening and In Vitro Identification of Hyperuricemia-Inhibiting Peptides fromFoods (Basel, Switzerland) · 2025Article
- A comprehensive analysis of trends in the burden of gout in China and globally from 1990 to 2021.Scientific reports · 2025Article
- Serum uric acid reduction through SGLT2 inhibitors: evidence from a systematic review and meta-analysis.Frontiers in pharmacology · 2025Article
- Transport mechanism and structural pharmacology of human urate transporter URAT1.Cell research · 2024Article
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Authors and funding
9 authors.
Funding
Abstract
Urate, the physiological form of uric acid and a potent antioxidant in serum, plays a pivotal role in scavenging reactive oxygen species. Yet excessive accumulation of urate, known as hyperuricemia, is the primary risk factor for the development of gout. The high-capacity urate transporter GLUT9 represents a promising target for gout treatment. Here, we present cryo-electron microscopy structures of human GLUT9 in complex with urate or its inhibitor apigenin at overall resolutions of 3.5 Å and 3.3 Å, respectively. In both structures, GLUT9 exhibits an inward open conformation, wherein the substrate binding pocket faces the intracellular side. These structures unveil the molecular basis for GLUT9's substrate preference of urate over glucose, and show that apigenin acts as a competitive inhibitor by occupying the substrate binding site. Our findings provide critical information for the development of specific inhibitors targeting GLUT9 as potential therapeutics for gout and hyperuricemia.
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