ArticleCell discovery2025
Molecular mechanisms of urate transport by the native human URAT1 and its inhibition by anti-gout drugs.
Article in Cell discovery, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Nucleotide Metabolism in Health and Disease.MedComm · 2026Review
- Pomegranate Peel Polyphenol Extract Ameliorates Hyperuricemia by Inhibiting Uric Acid Synthesis and Reabsorption.Chemical biology & drug design · 2026Article
- Development and validation of a risk models for gout in patients with diabetic kidney disease.BMC endocrine disorders · 2026Article
- Gut microbiota-associated N-Acetyl-L-leucine mediates fructose-induced hyperuricemia via the P300-URAT1 pathway.NPJ science of food · 2026Article
- Urate transporters: Structural mechanisms and therapeutic opportunities in drug development.Acta pharmaceutica Sinica. B · 2026Article
- A Novel Dual URAT1/GLUT9 Inhibitor Reduces Hyperuricemia by Enhancing Uric Acid Excretion and Attenuating Renal Fibrosis.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Enhancing therapeutic strategies and drug development for patients with kidney disease.Expert opinion on drug safety · 2026Review
- URAT1 and GLUT9 as drug targets in gout: progress in transporter-directed therapies and delivery technologies.Inflammopharmacology · 2025Review
- Antihyperuricemic Effects ofInternational journal of molecular sciences · 2025Article
- Discovery of multi-target anti-gout agents from Eurycoma longifolia Jack through phenotypic screening and structural optimization.Nature communications · 2025Article
- Extra-renal role of urate transporter-1 in diabetes.World journal of diabetes · 2025Review
- Molecular basis of the urate transporter URAT1 inhibition by gout drugs.Nature communications · 2025Article
- Article
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Authors and funding
16 authors.
Funding
Abstract
Gout, a common and painful disease, stems from hyperuricemia, where elevated blood urate levels lead to urate crystal formation in joints and kidneys. The human urate transporter 1 (hURAT1) plays a critical role in urate homeostasis by facilitating urate reabsorption in the renal proximal tubule, making it a key target for gout therapy. Pharmacological inhibition of hURAT1 with drugs such as dotinurad, benzbromarone, lesinurad, and verinurad promotes urate excretion and alleviates gout symptoms. Here, we present cryo-electron microscopy structures of native hURAT1 bound with these anti-gout drugs in the inward-open state, and with urate in inward-open, outward-open, and occluded states. Complemented by mutagenesis and cell-based assays, these structures reveal the mechanisms of urate reabsorption and hURAT1 inhibition. Our findings elucidate the molecular basis of urate transport and anti-gout medication action and provide a structural framework for the rational design of next-generation therapies for hyperuricemia and gout.
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