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TitleMechanisms of urate transport and uricosuric drugs inhibition in human URAT1.
Journal, issue, pagesNat Commun, Vol. 16, Issue 1, Page 1512, Year 2025
Publish dateFeb 10, 2025
AuthorsWenjun Guo / Miao Wei / Yunfeng Li / Jiaxuan Xu / Jiahe Zang / Yuezhou Chen / Lei Chen /
PubMed AbstractHigh urate levels in circulation lead to the accumulation of urate crystals in joints and ultimately inflammation and gout. The reabsorption process of urate in the kidney by the urate transporter ...High urate levels in circulation lead to the accumulation of urate crystals in joints and ultimately inflammation and gout. The reabsorption process of urate in the kidney by the urate transporter URAT1 plays a pivotal role in controlling serum urate levels. Pharmacological inhibition of URAT1 by uricosuric drugs is a valid strategy for gout management. Despite the clinical significance of URAT1, its structural mechanism and dynamics remain incompletely understood. Here, we report the structures of human URAT1 (hURAT1) in complex with substrate urate or inhibitors benzbromarone and verinurad at resolution ranges from 3.0 to 3.3 Å. We observe urate in the central substrate-binding site of hURAT1 in the outward-facing conformation and urate is wrapped in the center of hURAT1 by five phenylalanines and coordinated by two positively charged residues on each side. Uricosuric compounds benzbromarone and verinurad occupy the urate-binding site of hURAT1 in the inward-facing conformation. Structural comparison between different conformations of hURAT1 reveals the rocker-switch-like mechanism for urate transport. Benzbromarone and verinurad exert their inhibitory effect by blocking not only the binding of urate but also the structural isomerization of hURAT1.
External linksNat Commun / PubMed:39929841 / PubMed Central
MethodsEM (single particle)
Resolution3.0 - 3.26 Å
Structure data

60823

9irw

EMDB-60823, PDB-9irw:
Structure of human URAT1 bound with urate
Method: EM (single particle) / Resolution: 3.26 Å

60824

9irx

EMDB-60824, PDB-9irx:
Structure of human URAT1 bound with benzbromarone
Method: EM (single particle) / Resolution: 3.0 Å

60825

9iry

EMDB-60825, PDB-9iry:
Structure of human URAT1 bound with verinurad
Method: EM (single particle) / Resolution: 3.2 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

Source
  • homo sapiens (human)
KeywordsTRANSPORT PROTEIN / SLC22 / urate / gout / benzbromarone / Verinurad

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