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TitleStructural Basis for Inhibition of Urate Reabsorption in URAT1.
Journal, issue, pagesJACS Au, Vol. 5, Issue 3, Page 1308-1319, Year 2025
Publish dateMar 24, 2025
AuthorsJunping Fan / Wenjun Xie / Han Ke / Jing Zhang / Jin Wang / Haijun Wang / Nianxin Guo / Yingjie Bai / Xiaoguang Lei /
PubMed AbstractThe urate transporter 1 (URAT1) is the primary urate transporter in the kidney responsible for urate reabsorption and, therefore, is crucial for urate homeostasis. Hyperuricemia causes the common ...The urate transporter 1 (URAT1) is the primary urate transporter in the kidney responsible for urate reabsorption and, therefore, is crucial for urate homeostasis. Hyperuricemia causes the common human disease gout and other pathological consequences. Inhibition of urate reabsorption through URAT1 has been shown as a promising strategy in alleviating hyperuricemia, and clinical and preclinical drug candidates targeting URAT1 are emerging. However, how small molecules inhibit URAT1 remains undefined, and the lack of accurate URAT1 complex structures hinders the development of better therapeutics. Here, we present cryoelectron microscopy structures of a humanized rat URAT1 bound with benzbromarone, lingdolinurad, and verinurad, elucidating the structural basis for drug recognition and inhibition. The three small molecules reside in the URAT1 central cavity with different binding modes, locking URAT1 in an inward-facing conformation. This study provides mechanistic insights into the drug modulation of URAT1 and sheds light on the rational design of potential URAT1-specific therapeutics for treating hyperuricemia.
External linksJACS Au / PubMed:40151250 / PubMed Central
MethodsEM (single particle)
Resolution3.2 - 3.5 Å
Structure data

61155

9j5w

EMDB-61155, PDB-9j5w:
Cryo-EM Structure of URAT1 in Complex with Benzbromarone
Method: EM (single particle) / Resolution: 3.2 Å

61156

9j5x

EMDB-61156, PDB-9j5x:
Cryo-EM Structure of URAT1 in Complex with Lingolinurad
Method: EM (single particle) / Resolution: 3.44 Å

61157

9j5z

EMDB-61157, PDB-9j5z:
Cryo-EM Structure of URAT1 in Complex with Verinurad
Method: EM (single particle) / Resolution: 3.5 Å

Chemicals

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

PDB-1eap:
CRYSTAL STRUCTURE OF A CATALYTIC ANTIBODY WITH A SERINE PROTEASE ACTIVE SITE

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

Source
  • rattus norvegicus (Norway rat)
KeywordsMEMBRANE PROTEIN / Inhibitor / complex

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