Disease relevance of NSC56052

• The more active analogues (ED50), including 4-pyri-dylpyrimidines 4a (38), 4b (47), and 4g (49) and 2-hydroxypyrimidine 8r (43), were then tested against adjuvant-induced edema in the rat [1].

High impact information on NSC56052

• Under anaerobic conditions, carcinogenic 2-nitrofluorene, 4-nitrobiphenyl, and 1-nitro-naphthalene were reduced to the corresponding hydroxylamines and amines, whereas the carcinogenic 1-nitropyrene was reduced only to the corresponding amine by liver cytosol in the presence of 2-hydroxypyrimidine, an electron donor of aldehyde oxidase [2].
• We tested the effect of 2-amino-5-bromo-6 phenyl-4 pyrimidinol (ABPP), an interferon (IFN) inducer, on NK cell cytotoxicity in various tissues of athymic and euthymic rats [3].
• The 9,000g supernatant of ciliary body, retinal pigment epithelium-choroid, iris, retina and cornea, but not lens, exhibited reductase activity under anaerobic conditions when supplemented with 2-hydroxypyrimidine, an electron donor of aldehyde oxidase [4].
• First, classical AOX electron donor substrates (benzaldehyde, 2-hydroxypyrimidine, and N-methylnicotinamide) dramatically increase the rate of formation of IMI metabolites [5].
• However, when fenthion sulfoxide was incubated with liver cytosol in the presence of 2-hydroxypyrimidine, an electron donor of aldehyde oxidase, the extract of the incubation mixture exhibited antiandrogenic activity [6].

Biological context of NSC56052

• Zebularine (2(1H)-pyrimidinone riboside, Zeb), a synthetic analogue of cytidine that is a potent inhibitor of cytidine deaminase, has been recently identified as a general inhibitor of DNA methylation [7].

Anatomical context of NSC56052

• The cytosol by itself exhibited some nitroreductase activities, which were markedly enhanced by addition of an electron donor of aldehyde oxidase, i.e., N1-methylnicotinamide or 2-hydroxypyrimidine [2].
• The metabolism of diazinon, an organo-phosphorothionate pesticide, to diazoxon and pyrimidinol has been studied in incubations with hepatic microsomes from control Sprague-Dawley (SD) rats or SD rats treated with different P450-specific inducers (phenobarbital, dexamethasone, beta-napthoflavone, and pyrazole) [8].

Associations of NSC56052 with other chemical compounds

• This enzyme efficiently utilized 2-hydroxypyrimidine and benzaldehyde as electron donors while N1-methylnicotinamide was 40 times less effective than 2-hydroxypyrimidine [9].
• NF was reduced to 2-aminofluorene by hamster skin cytosol in the presence of 2-hydroxypyrimidine, 4-hydroxypyrimidine, N(1)-methylnicotinamide, or benzaldehyde, but not hypoxanthine or xanthine [10].
• The 2-hydroxypyrimidine-dependent cytosolic activity exhibited marked strain differences, unlike the NADPH-dependent microsomal activity [11].
• However, a marked decrease of MPTP lactam as well as MP 2-pyridone and a concomitant increase of MPP(+) were caused by coinfusion of 2-hydroxypyrimidine (2-OH PM), a competitive inhibitor of AO, into Jcl:Wistar rat liver [12].

Analytical, diagnostic and therapeutic context of NSC56052

• Serum activity was assessed in as close to physiological conditions as possible (at pH 7.4, 150 mM NaCl and 37 degrees C with 50 microM diazoxon as substrate) and by quantifying pyrimidinol formation using high-performance liquid chromatography [13].

References