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A case of acute renal failure after exercise with renal hypouricemia demonstrated compound heterozygous mutations of uric acid transporter 1

Clinical and Experimental Nephrology, 2011
Familial renal hypouricemia is a hereditary disease characterized by extraordinary high renal uric acid (UA) clearance and is associated with acute renal failure (ARF). A 17-year-old Japanese male developed ARF after anerobic exercise. Renal function improved completely after approximately 2 weeks of hydration treatment.
Ayami, Ochi   +8 more
openaire   +2 more sources

Discovery of potent and orally bioavailable inhibitors of Human Uric Acid Transporter 1 (hURAT1) and binding mode prediction using homology model

Bioorganic & Medicinal Chemistry Letters, 2016
This Letter describes the discovery of a series of potent inhibitors of Human Uric Acid Transporter 1 (hURAT1). Lead generation and optimization via 3D pharmacophore analysis resulted in compound 41. With an IC50 of 33.7nM, 41 also demonstrated good oral bioavailability in rat (74.8%) and displayed a consistent PK profile across all species tested (rat,
Jianbiao, Peng   +10 more
openaire   +2 more sources

Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout

Bioorganic & Medicinal Chemistry Letters, 2019
As a part of our ongoing research to develop novel URAT1 inhibitors, 19 compounds (1a-1s) based on carboxylic acid bioisosteres were synthesized and tested for in vitro URAT1 inhibitor activity (IC50). The structure-activity relationship (SAR) exploration led to the discovery of a highly potent novel URAT1 inhibitor 1g, which was 225-fold more potent ...
Jing-Wei, Wu   +6 more
openaire   +2 more sources

Structural similarity-based search for glinides exhibiting cis- and trans-inhibitory activity toward uric acid transporter 1

Molecular Pharmacology
Various types of drugs can affect serum urate levels as side effects. Although these drugs are used to treat different diseases, they might share a structural component that acts on a common target to affect urate levels. Human urate transporter 1 (URAT1) plays an essential role in urate reabsorption at the renal proximal tubule and thus might be a ...
Misa Sayama   +5 more
openaire   +2 more sources

Proline-derived quinoline formamide compounds as human urate transporter 1 inhibitors with potent uric acid-lowering activities

European Journal of Medicinal Chemistry
We report the design and synthesis of a series of proline-derived quinoline formamide compounds as human urate transporter 1 (URAT1) inhibitors via a ligand-based pharmacophore approach. Structure-activity relationship studies reveal that the replacement of the carboxyl group on the polar fragment with trifluoromethanesulfonamide and substituent ...
Shengnan Li   +15 more
openaire   +2 more sources

Uric Acid Transport, Transporters, and Their Pharmacological Targeting

Acta Physiologica, 2023
Orson W. Moe, Emmanuel A Adomako
exaly  

Function of Uric Acid Transporters and Their Inhibitors in Hyperuricaemia

Frontiers in Pharmacology, 2021
Xiao-ming Meng, Heng Wang, Juan Jin
exaly  

Sodium-Glucose Co-Transporter-2 (SGLT-2) Inhibitors and Uric Acid: More Good News!

Journal of Diabetes and Its Complications, 2023
Manfredi Rizzo   +2 more
exaly  

Human uric acid transporter 1 gene analysis in familial renal hypo‐uricemia associated with exercise‐induced acute renal failure

Pediatrics International, 2007
Yasufumi, Ohtsuka   +6 more
openaire   +2 more sources

The Effect of Polymorphism of Uric Acid Transporters on Uric Acid Transport

Journal of Nephrology, 2019
Yazhuo Li, Fang Zhao, Rui Liu
exaly  

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