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Structure paper

TitleMolecular mechanism of drug inhibition of URAT1.
Journal, issue, pagesNat Commun, Vol. 16, Issue 1, Page 6551, Year 2025
Publish dateJul 16, 2025
AuthorsZhuoya Yu / Tuo Hu / Jiawei Su / Jun Zhao / Renjie Li / Qiao Ma / Qihao Chen / Qinru Bai / Yanli Dong / Pu Yuan / Na Li / Xuejun Cai Zhang / Yan Zhao /
PubMed AbstractHyperuricemia, characterized by elevated serum urate levels, is a key factor in the pathogenesis of gout. URAT1 is essential for renal urate reabsorption and has emerged as a critical therapeutic ...Hyperuricemia, characterized by elevated serum urate levels, is a key factor in the pathogenesis of gout. URAT1 is essential for renal urate reabsorption and has emerged as a critical therapeutic target for managing hyperuricemia. However, the precise transport mechanism and the inhibitory effects of uricosuric drugs on URAT1 remain unclear. Here, we present structures of the double-mutant rat homolog of URAT1 in complex with its substrate urate, and the clinical drugs benzbromarone, lesinurad, verinurad, and sulfinpyrazone. The urate-bound structure elucidates key residues involved in recognizing urate, while the structures bound with drugs clearly demonstrate the distinct binding mode of each drug with URAT1. These drugs stabilize URAT1's inward-facing state, blocking conformational transitions. Additionally, critical interactions essential for its conformational transition are identified. These findings provide a molecular framework for understanding the physiological function of URAT1 and for developing more efficacious therapies to treat hyperuricemia.
External linksNat Commun / PubMed:40670375 / PubMed Central
MethodsEM (single particle)
Resolution3.47 - 3.51 Å
Structure data

61191

9j72

EMDB-61191, PDB-9j72:
Cryo-EM structure of URAT1 in complex with uric acid
Method: EM (single particle) / Resolution: 3.47 Å

61192

9j73

EMDB-61192, PDB-9j73:
Cryo-EM structure of URAT1 in complex with benzbromarone
Method: EM (single particle) / Resolution: 3.5 Å

61194

9j75

EMDB-61194, PDB-9j75:
Cryo-EM structure of URAT1 in complex with verinurad
Method: EM (single particle) / Resolution: 3.5 Å

61195

9j76

EMDB-61195, PDB-9j76:
Cryo-EM structure of URAT1 in complex with sulfinpyrazone
Method: EM (single particle) / Resolution: 3.51 Å

Chemicals

ChemComp-URC:
URIC ACID

ChemComp-R75:
[3,5-bis(bromanyl)-4-oxidanyl-phenyl]-(2-ethyl-1-benzofuran-3-yl)methanone / antiarrhythmic, inhibitor*YM

PDB-1aij:
PHOTOSYNTHETIC REACTION CENTER FROM RHODOBACTER SPHAEROIDES IN THE CHARGE-NEUTRAL DQAQB STATE

PDB-1eay:
CHEY-BINDING (P2) DOMAIN OF CHEA IN COMPLEX WITH CHEY FROM ESCHERICHIA COLI

Source
  • rattus norvegicus (Norway rat)
KeywordsTRANSPORT PROTEIN / protein structure / STRUCTURAL PROTEIN

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