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Xanthine oxidoreductase and its inhibitors: relevance for gout
Clinical Science, 2016Xanthine oxidoreductase (XOR) is the rate-limiting enzyme in purine catabolism and converts hypoxanthine to xanthine, and xanthine into uric acid. When concentrations of uric acid exceed its biochemical saturation point, crystals of uric acid, in the form of monosodium urate, emerge and can predispose an individual to gout, the commonest form of ...
Richard O, Day +4 more
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Bioorganic Chemistry, 2022
Xanthine oxidoreductase (XOR) is a clinically validated target for the treatment of hyperuricemia and gout. A series of novel 1,2,4-triazoles were identified as potent XO inhibitors via a fused-pharmacophore strategy based on the interaction modes of febuxostat and topiroxostat. Among them, compound 7i showed an IC50 value of 0.20 nM against XOR, which
Yajun Yang +10 more
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Xanthine oxidoreductase (XOR) is a clinically validated target for the treatment of hyperuricemia and gout. A series of novel 1,2,4-triazoles were identified as potent XO inhibitors via a fused-pharmacophore strategy based on the interaction modes of febuxostat and topiroxostat. Among them, compound 7i showed an IC50 value of 0.20 nM against XOR, which
Yajun Yang +10 more
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Archives of Toxicology, 2014
The present study was performed to elucidate the underlying mechanism of transitional cell tumors found in the carcinogenicity testing of topiroxostat, a xanthine oxidoreductase inhibitor, in which topiroxostat was orally given to F344 rats at 0.3, 1, and 3 mg/kg for 2 years.
Takeo, Shimo +5 more
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The present study was performed to elucidate the underlying mechanism of transitional cell tumors found in the carcinogenicity testing of topiroxostat, a xanthine oxidoreductase inhibitor, in which topiroxostat was orally given to F344 rats at 0.3, 1, and 3 mg/kg for 2 years.
Takeo, Shimo +5 more
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Anti‐hyperuricemia activity and toxicity prediction of a novel xanthine oxidoreductase inhibitor
Biomedical Chromatography, 2019AbstractA potent xanthine oxidoreductase inhibitor (LS087) was recently proved to exhibit a similar hypouricemic potency to febuxostat. A hyperuricemia model induced by potassium oxonate and hypoxanthine was proposed in specific pathogen‐free male Kunming mice, and the serum urea nitrogen, creatinine and uric acid levels were measured after oral ...
Liping Zhou +5 more
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Study on species differences in nephropathy induced by FYX-051, a xanthine oxidoreductase inhibitor
Archives of Toxicology, 2010To clarify the toxicological aspects of FYX-051, a xanthine oxidoreductase inhibitor, which is currently being developed as a therapeutic agent against gout and hyperuricemia, we performed the study focused on species differences in FYX-051-induced nephropathy.
Takeo, Shimo +4 more
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Biomedicine and PharmacotherapyHyperuricemia is with growing incidence and of high risk to develop into gout and other metabolic diseases. The key enzyme catalyzing uric acid synthesis, xanthine oxidoreductase (XOR) is a vital target for anti-hyperuricemic drugs, while XOR inhibitors characterized as both potent and safe are currently in urgent need.
Xuechen Li
exaly +3 more sources
Radiation Research, 2002
The xanthine oxidoreductase (XOD) system, which consists of xanthine dehydrogenase (XDH) and xanthine oxidase (XO), is one of the major sources of free radicals in biological systems. The XOD system is present predominantly in the normal tissues as XDH. In damaged tissues, XDH is converted into XO, the form that generates free radicals.
M, Srivastava, D, Chandra, R K, Kale
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The xanthine oxidoreductase (XOD) system, which consists of xanthine dehydrogenase (XDH) and xanthine oxidase (XO), is one of the major sources of free radicals in biological systems. The XOD system is present predominantly in the normal tissues as XDH. In damaged tissues, XDH is converted into XO, the form that generates free radicals.
M, Srivastava, D, Chandra, R K, Kale
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Rheumatology International, 2015
Increase in thyroid stimulating hormone (TSH) levels over the upper normal limit has been reported in a small percentage of patients treated with febuxostat in clinical trials, but a mechanistic explanation is not yet available. In an observational parallel longitudinal cohort study, we evaluated changes in TSH levels in patients with gout at baseline ...
Fernando, Perez-Ruiz +5 more
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Increase in thyroid stimulating hormone (TSH) levels over the upper normal limit has been reported in a small percentage of patients treated with febuxostat in clinical trials, but a mechanistic explanation is not yet available. In an observational parallel longitudinal cohort study, we evaluated changes in TSH levels in patients with gout at baseline ...
Fernando, Perez-Ruiz +5 more
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[Inhibitors of xanthine oxidoreductase].
Nihon rinsho. Japanese journal of clinical medicine, 2008Inhibitors of xanthine oxidoreductase decrease production of uric acid, thus they act as hypouricemic drugs. Allopurinol, a prototypical xanthine oxidoreductase inhibitor, has been widely prescribed for treatment of gout and hyperuricemia. However, severe side effects of allopurinol may occur in patients with renal insufficiency.
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Can Xanthine Oxidoreductase Inhibitor Protect Kidney against Progressive Injury?
Journal of Developing Drugs, 2012Hyperuricemia has been shown to associate with high incidence of cardiovascular or kidney disease [1,2] and the beneficial effect of the treatment with allopurinol has been shown in hyperuricemic chronic kidney disease (CKD) patients [3]. Moreover, recent investigations have demonstrated that monosodium urate crystals activate natural immune system ...
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