An Extremely Potent Inhibitor of Xanthine Oxidoreductase

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FYX-051: a novel and potent hybrid-type inhibitor of xanthine oxidoreductase.

4-[5-(Pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile (FYX-051) is a potent inhibitor of bovine milk xanthine oxidoreductase (XOR). Steady-state kinetics study showed that it initially behaved as a competitive-type inhibitor with a K(i) value of 5.7 × 10(-9) M, then after a few minutes it formed a tight complex with XOR via a Mo-oxygen-carbon atom covalent linkage, as reported previ...

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Xanthine oxidoreductase is an endogenous regulator of cyclooxygenase-2.

Xanthine oxidoreductase (XOR) is the enzyme responsible for the final step in purine degradation resulting in the generation of uric acid. Here we have generated mice deficient in XOR. As expected, these animals lack tissue XOR activity and have low to undetectable serum levels of uric acid. Although normal at birth, XOR-/- mice fail to thrive after 10 to 14 days, and most die within the first ...

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Regulation of xanthine oxidoreductase by intracellular iron.

Xanthine oxidoreductase (XOR) may produce reactive oxygen species and play a role in ischemia-reperfusion injury. Because tissue iron levels increase after ischemia, and because XOR contains functionally critical iron-sulfur clusters, we studied the effects of intracellular iron on XOR expression. Ferric ammonium citrate and FeSO(4) elevated intracellular iron levels and increased XOR activity ...

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Onion (Allium Cepa) contains high levels of flavonoids. Although there are many studies indicating the inhibitory effects of flavonoids on xanthine oxidase, there is no report on the effect of onion on this enzyme. Therefore, in the present study, the inhibitory effects of onion on xanthine oxidase are investigated. Fresh filtered juice of onion was prepared and its inhibitory effect on guine...

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ژورنال

عنوان ژورنال: Journal of Biological Chemistry

سال: 2003

ISSN: 0021-9258

DOI: 10.1074/jbc.m208307200