Potent human uric acid transporter 1 inhibitors: in vitro and in vivo metabolism and pharmacokinetic studies [PDF]
Michael F Wempe,1 Janet W Lightner,2 Bettina Miller,1 Timothy J Iwen,1 Peter J Rice,1 Shin Wakui,3 Naohiko Anzai,4 Promsuk Jutabha,4 Hitoshi Endou51Department of Pharmaceutical Sciences, School of Pharmacy, University of Colorado Denver, Anschutz Medical
Wempe MF +8 more
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Developing Potent Human Uric Acid Transporter 1 (hURAT1) Inhibitors [PDF]
The kidneys are a vital organ in the human body. They serve several purposes including homeostatic functions such as regulating extracellular fluid volume and maintaining acid-base and electrolyte balance and are essential regarding the excretion of metabolic waste.
Wempe, Michael F. +8 more
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Structural Insights into the Atomistic Mechanisms of Uric Acid Recognition and Translocation of Human Urate Anion Transporter 1 [PDF]
Abstract Background: Human urate transporter 1 (hURAT1) is the most pivotal therapeutic target for treating hyperuricemia. However, the molecular interactions between uric acid and URAT1 are still unknown due to lack of structural details.
Ze’an Zhao +12 more
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Virtual screening and activity evaluation of human uric acid transporter 1 (hURAT1) inhibitors. [PDF]
Alphafold2 was used to predict URAT1 protein structure, then the docking sites were identified, and three hit compounds were obtained through virtual screening and bioactivity verification.
Yang Y +6 more
europepmc +3 more sources
Impact of Renal Impairment on the Pharmacodynamic and Pharmacokinetic Profiles of Epaminurad, a Novel Uric Acid Transporter 1 Inhibitor. [PDF]
ABSTRACTEpaminurad, a novel uricosuric agent, exhibits potent inhibitory activity against the human uric acid transporter. This study aimed to investigate the effects of renal function and food intake on the pharmacokinetic, pharmacodynamic, and safety characteristics of 9 mg epaminurad.
Park SY, Hwang JG, Cho SK, Park MK.
europepmc +4 more sources
Human urate transporter 1 (hURAT1) is the most pivotal therapeutic target for hyperuricemia. Due to a lack of crystal structure information, the atomic structure of URAT1 is not clearly understood. In this study, a multiple sequence alignment was performed, and K393, a positively charged residue in transmembrane domain (TMD) 8, was observed to be ...
Qunsheng Lan +7 more
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Sodium-Hydrogen Exchanger Regulatory Factor-1 Interacts with Mouse Urate Transporter 1 to Regulate Renal Proximal Tubule Uric Acid Transport [PDF]
Sodium-hydrogen exchanger regulatory factor-1-deficient (NHERF-1(-/-)) mice demonstrate increases in the urinary excretion of phosphate, calcium, and uric acid associated with interstitial deposition of calcium in the papilla of the kidney. These studies examine the role of NHERF-1 in the tubular reabsorption of uric acid and regulation of mouse urate ...
Rochelle, Cunningham +11 more
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Association of the human urate transporter 1 with reduced renal uric acid excretion and hyperuricemia in a German Caucasian population [PDF]
AbstractObjectiveHuman urate transporter 1 (hURAT1) is a member of the organic anion transporter family (SLC22A12) that mainly regulates tubular urate reabsorption. Loss‐of‐function mutations result in idiopathic hypouricemia. The present case–control study was designed to analyze whether hURAT1 might also be a candidate gene for hyperuricemia with ...
Juergen, Graessler +6 more
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SLC2A9 is a high-capacity urate transporter in humans [PDF]
Background Serum uric acid levels in humans are influenced by diet, cellular breakdown, and renal elimination, and correlate with blood pressure, metabolic syndrome, diabetes, gout, and cardiovascular disease. Recent genome-wide association scans have
Doblado M +241 more
core +1 more source
We have read with interest the letter by Dr Wang [1] commenting on our article ‘The association of uric acid with mortality modifies at old age: data from the uric acid right for heart health (URRAH) study’ [2].
Borghi C +5 more
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