Table 2.
Urate transporters and their characteristics related to launched therapies for hyperuricemia
| Transporter | Function | Location | Inhibitors |
|---|---|---|---|
| SLC22A12 (URAT1) | Mediating the reabsorption of UA from the renal tubular fluid back into the blood. | Apical membrane of the proximal tubule cells | Lesinurad; Benzbromarone; Arhalofenate (MBX201); Dotinurad; Tranilast |
| SLC2A9 (GLUT9) | Mediating the transport of urate from the tubular cells back into circulation, influencing renal urate reabsorption. | Apical and basolateral membrane of the proximal tubule | Benzbromarone; Tranilast |
| ABCG2 (BCRP) | Secretion of urate into the tubular lumen, facilitating renal urate excretion. | Apical membrane of renal tubules and intestine epithelial cells | Topiroxostat |
| SLC22A6 (OAT1) | Uptake of urate from the interstitial space into the tubular cells, contributing to urate secretion. | Basolateral side of the proximal tubule | Probenecid |
| SLC22A8 (OAT3) | Uptake of urate into renal tubular cells, facilitating urate secretion. | Basolateral membrane of the proximal tubule | Probenecid |
| SLC22A11 (OAT4) | Apical uptake of urate into renal tubular cells, potentially participating in urate reabsorption. | Apical side of the proximal tubule | Lesinurad; Arhalofenate (MBX201) |
| SLC17A1 (NPT1) | Secretion of urate into the tubular lumen, influencing renal urate excretion. | Apical membrane of the proximal tubule | |
| SLC17A3 (NPT4) | Secretion of urate into the tubular lumen, contributing to renal urate excretion. | Apical side of the renal proximal tubule | |
| PDZK1 | PDZK1 acts as a scaffold protein, regulating the activity of various transport proteins in the proximal tubules, including URAT1 and NPT1. It enhances the UA reabsorption capacity of URAT1 and may influence the function of ABCG2. | Apical membrane of the proximal tubular in kidney |