Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:6.3.4.6 (urease)
7,490 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

We examined several compounds for their mechanisms of inhibition with the nickel-containing active site of homogeneous Klebsiella aerogenes urease. Thiolate anions competitively inhibit urease and directly interact with the metallocenter, as shown by the pH dependence of inhibition and by UV-visible absorbance spectroscopic studies. Cysteamine, which possesses a cationic beta-amino group, exhibited a high affinity for urease (Ki = 5 microM), whereas thiolates containing anionic carboxyl groups were uniformly poor inhibitors. Phosphate monoanion competitively inhibits a protonated form of urease with a pKa of less than 5. Both the thiolate and phosphate inhibition results are consistent with charge repulsion by an anionic group in the urease active site. Acetohydroxamic acid (AHA) was shown to be a slow-binding competitive inhibitor of urease. This compound forms an initial E.AHA complex which then undergoes a slow transformation to yield an E.AHA* complex; the overall dissociation constant of AHA is 2.6 microM. Phenylphosphorodiamidate, also shown to be a slow-binding competitive inhibitor, possesses an overall dissociation constant of 94 pM. The tight binding of phenylphosphorodiamidate was exploited to demonstrate the presence of two active sites per enzyme molecule. Urease contains 4 mol of nickel/mol enzyme, hence there are two nickel ions/catalytic unit. Each of the two slow-binding inhibitors are proposed to form complexes in which the inhibitor bridges the two active site nickel ions. The inhibition results obtained for K. aerogenes urease are compared with inhibition studies of other ureases and are interpreted in terms of a model for catalysis proposed for the jack bean enzyme (Dixon, N.E., Riddles, P.W., Gazzola, C., Blakely, R.L., and Zerner, B. (1980) Can. J. Biochem. 58, 1335-1344).
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PMID:Competitive inhibitors of Klebsiella aerogenes urease. Mechanisms of interaction with the nickel active site. 267 18

A procedure is described for the analysis of serum cations and uremic toxins by simultaneous conductivity (CD) and ultraviolet (UV) photometric detection and using phosphoric acid as the eluent. In addition, studies were made on the determination of urea in serum using immobilized urease, and on the simultaneous determination of cationic and anionic compounds. The ammonium ion produced from urea by immobilized urease was determined by CD. No significant differences in amounts were found between the present method and conventional colorimetric methods. There was no significant reduction in immobilized urease activity after two months of continuous use. Simultaneous analysis of cationic and anionic compounds in serum was performed by switching valves in order to change the eluents and to change the channel to the analytical column. No marked base-line variation was observed and satisfactory recovery of anions was achieved.
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PMID:Simultaneous determination of serum cations, anions and uremic toxins by ion chromatography using an immobilized enzyme. 408 36

In two experiments with one dairy cow each the utilisation of urea-N after its ruminal or duodenal infusion was comparatively investigated on two crude protein levels and different urease activities in the rumen. The rations contained 9.6 (I) and 14.3 (II) g crude plant protein/100 g dry matter. After completed adaptation 50 g urea were daily infused in the rumen (R, via cannula) in 3 h resp. the duodemun (D, distal cannula of the reentrance cannula) in 6 h with the morning and evening feeding. In experiment II the urease blocker phosphoric acid phenylester diamide (D/PPD) was applied in an additional experiment synchronously with the duodenal urea application. On the first measuring day in each case the urea in the morning feeding was labelled with 17.4 atom-% 15N-excess (15N'). Measuring results in the sequence I R, I D, II R, II D, II D/PPD: 15N'-passage rate at the duodenum within 72 h in the TCA-soluble N-fraction 29, 18, 24, 13 and 16, in the TCA-precipitable N-fraction 59, 25, 41, 11 and 5% of the application, 15N'-excretion within 96 h in milk protein 6.8, 4.2, 4.6, 3.4 and 1.9, in faeces 20, 12, 19, 8 and 4, in urine 20, 32, 34, 56 and 75% of the application, 15N-balance 59, 56, 47, 36 and 21% of the application, passage rate of non-NH3-N in the duodenum 131, 118, 96, 107 and 99% of the total N-intake. After ruminal infusion there always was a higher NH3-concentration in the rumen and 15N-frequencies in the rumen proteins. One can conclude that urea-N that gets into the intestines is to a low degree used for duodenal protein supply as directly utilisable urea-N from the ration in the rumen. The difference increases with the protein content of the ration and the inhibition of rumen urease. The urea N-balance is to a considerably smaller degree influenced by the place of urea infusion particularly at a low level of N-supply, which is due to a better utilisation of the urea-N transported with intermediary metabolism from the intestines. The role of urease as a regulator of urea transport through the rumen wall cannot be corroborated.
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PMID:[Transport of urea nitrogen from the intestines into the stomach in dairy cows]. 652 64

Phosphate stones are divided in two groups: I. Infection stones = triple phosphate stones (struvite and carbonate apatite). II. Calcium phosphate stones = Hydroxy apatite. Ad I. For the formation of this stone, infection with urease-producing bacteria is essential. It is important to look for factors that cause infection and for metabolic abnormalities. Three possibilities for treatment are discussed: Acidifying the urine: orally with NH4NO3 or NH4Cl; dosage is possible up to 12 g a day (metabolic acidosis!). Irrigation for instance with Renacidin ; when using a nephrostomy-tube, one can start 5 days after the operation. It is important to look for fever and flank pain. Especially useful in cases with small residual stones. Reduction of phosphate excretion in urine ( Shorr -regimen). Some aluminium combinations reduce the intestinal phosphate absorption as a result of the formation of a nonabsorbable aluminium-phosphate combination. This can be combined with a low calcium- and phosphate diet. In several publications good results are shown. Also when using a less rigid regimen, satisfactory results are seen: decrease of the phosphate excretion from 30 to 17 mmol/24 h (own investigation). Urease-inhibitors result in a lower urine-pH and a decrease of the ammonium-concentration. there are only a few publications with results, but AHA seems able to reduce the stone size in 24% of the patients. Ad II. This stone is concerning formation and treatment much like the calcium oxalate stone. In case of an alkaline urine one must look for primary hyperparathyroidism and renal tubular acidosis.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Conservative therapy of phosphate calculi]. 653 26

Helicobacter pylori urease is a nickel-containing enzyme that hydrolyzes urea to bicarbonate and ammonia. Andrews et al. (J. Am. Chem. Soc. 1986, 108, 7124) have shown that amides and esters of phosphoric acid are slow, tight-binding inhibitors of urease isolated from jack bean. We show that 4-substituted phenyl phosphorodiamidates (4-R-PhOP(=O)(NH2)2) are slow-binding inhibitors of H. pylori urease with no evidence of kinetic saturation. Their second-order rates of inhibition ki are strongly correlated with phenol pKa (e.g. R = NO2, ki = 2.5 x 10(5) M-1s-1; R = OMe, ki = 1.2 x 10(4) M-1s-1). The Bronsted beta for inhibition is 0.4, similar to that of model system SN2(P) reactions. Based on these observations, we suggest that urease inhibition is covalent but reversible, involving a common phosphoacyl enzyme intermediate.
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PMID:Inhibition of Helicobacter pylori urease by phenyl phosphorodiamidates: mechanism of action. 764 8

1. Stable urea isotopes can be used to study urea kinetics in humans. The use of stable urea isotopes for studying urea kinetic parameters in humans on a large scale is hampered by the high costs of the labelled material. We devised a urea dilution for measurement of the distribution volume, production rate and clearance of urea in healthy subjects and renal failure patients using the inexpensive single labelled [13C]urea isotope with subsequent analysis by headspace chromatography-isotope ratio MS (GC-IRMS) of the [13C]urea enrichment. 2. The method involves measurement of the molar percentage excess of [13C]urea in plasma samples taken over a 4 h period after an intravenous bolus injection of [13C]urea. During the sample processing procedure, the plasma samples together with calibration samples containing a known molar percentage excess of [13C]urea are acidified with phosphoric acid to remove endogenous CO2, and are subsequently incubated with urease to convert the urea present in the plasma samples into CO2. The 13C enrichment of the generated CO2 is analysed by means of GC-IRMS. This method allows measurement of the molar percentage excess of [13C]urea to an accuracy of 0.02%. 3. Reproducibility studies showed that the sample processing procedure [within-run coefficient of variation (CV) < 2.8% and between-run CV < 8.8%] and the GC-IRMS analysis (within-day CV < 1.3% and between-day CV < 1.3%) could be repeated with good reproducibility. 4. In clinical urea kinetic studies in a healthy subject and in a renal failure patient without residual renal function, reproducible values of the distribution volume, production rate and clearance of urea were determined using minimal amounts of [13C]urea (25-50 mg). 5. Because only low [13C]urea enrichments are needed in this urea dilution method using GC-IRMS analysis, the costs of urea kinetic studies are reduced considerably, especially in patients with renal failure.
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PMID:Determination of urea kinetics by isotope dilution with [13C]urea and gas chromatography-isotope ratio mass spectrometry (GC-IRMS) analysis. 927 6

Purple acid phosphatases (PAPs) are a family of binuclear metalloenzymes that catalyze the hydrolysis of phosphoric acid esters and anhydrides. A PAP in sweet potato has a unique, strongly antiferromagnetically coupled Fe(III)-Mn(II) center and is distinguished from other PAPs by its increased catalytic efficiency for a range of activated and unactivated phosphate esters, its strict requirement for Mn(II), and the presence of a mu-oxo bridge at pH 4.90. This enzyme displays maximum catalytic efficiency (k(cat)/K(m)) at pH 4.5, whereas its catalytic rate constant (k(cat)) is maximal at near-neutral pH, and, in contrast to other PAPs, its catalytic parameters are not dependent on the pK(a) of the leaving group. The crystal structure of the phosphate-bound Fe(III)-Mn(II) PAP has been determined to 2.5-A resolution (final R(free) value of 0.256). Structural comparisons of the active site of sweet potato, red kidney bean, and mammalian PAPs show several amino acid substitutions in the sweet potato enzyme that can account for its increased catalytic efficiency. The phosphate molecule binds in an unusual tripodal mode to the two metal ions, with two of the phosphate oxygen atoms binding to Fe(III) and Mn(II), a third oxygen atom bridging the two metal ions, and the fourth oxygen pointing toward the substrate binding pocket. This binding mode is unique among the known structures in this family but is reminiscent of phosphate binding to urease and of sulfate binding to lambda protein phosphatase. The structure and kinetics support the hypothesis that the bridging oxygen atom initiates hydrolysis.
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PMID:Phosphate forms an unusual tripodal complex with the Fe-Mn center of sweet potato purple acid phosphatase. 1562 11

In order to establish an evaluation system for selection of winter wetland plants possessing high wastewater purification potentials in subtropics areas, designed sewage treatment experiments were carried out by introducing into the constructed wetlands 25 species of winter wetland plants. Cluster analysis was performed by including harmful environment-resistant enzyme and substrate enzyme activities into the commonly applied plant screening and assessment indexes system. The obtained results indicated that there were significant differences among the tested winter plants in their root length and vigor, leaf malonaldehyde (MDA), biomass, average nitrogen and phosphorus concentration and uptake, and urease and phosphoric acid enzyme activities in the root areas. Based on the established evaluation system, the tested plants were clustered into 3 groups. The plants in the 1st group possessing high purification potentials are Oenanthe javanica, Brassicacapestris, Juncus effusu, Saxifragaceae, Iris pseudoacorus, Osmanthus fragrans and Iris ensata; those in the 2nd group possessing moderate purification potentials are Brassica oleracea var acephala, Calendula officinalis, Aucuba japonica, Ligustrum lucidu, Beta vulgaris, Rhododendron simsii and Ilex latifolia; and those in the 3rd group with low purification potentials are Brassica oleracea var acephala, Calistephus chinensis, Rosa chinensis, Antirrhinums, Liriope palatyphylla, Zephyranthes candida, Fatshedera lizei, Petunia hybrida, Ilex quihoui, Dianthus caryophyllus and Loropetalum chinensis.
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PMID:[Selection of winter plant species for wetlands constructed as sewage treatment systems and evaluation of their wastewater purification potentials]. 2109 Feb 94

The course of recurrent urolithiasis was studied in 131 patients (64 females, 67 males, age 27-69 years). Before the start of 1-15-year followup the patients' condition was: after spontaneous elimination of the concrements, after extracorporeal shock-wave lithotripsy and/or percutaneous nephrolitholapaxy, after open surgical interventions, after surgery and spontaneous elimination of the concriments, after litholysis (patients with hyperuricemic urolithiasis). At the start of the follow-up 127 patients had no uroliths, 4 patients had bilateral concrements. The group of patients free of uroliths consisted of 33 patients with hyperuricemic urolithiasis, 52--with calcium-oxalate, 42--with magnesium-ammonium-phosphate form of the disease. As shown by follow-up ultrasound and x-ray examinations, each of these patients had 1 to 7 recurrent concrements. Infrared spectrophotometry and x-ray diffraction determined chemical composition of both primary and 352 recurrent concrements. The patients were also examined with biochemical, microbiological methods, urine clinical examination was made. Possibility, metabolic and microbiological evidence for changes in urolithogenesis type in patients with different forms of the disease were found. In hyperuricemic urolithiasis recurrent concrements can be calcium-oxalate and phosphate, in calcium-oxalate urolithiasis--phosphate. Transformation of magnesium-ammonium-phosphate urolithiasis into hyperuricemic or calcium-oxalate urolithiasis was observed. Changes in the form of the disease more frequently occur in hyperuricemic and calcium-oxalate urolithiasis than in phosphate one. Phosphate concrements form less frequently in patients with hyperuricemic urolithiasis. One kidney can simultaneously contain hyperuricemic or calcium-oxalate concrement while the contralateral kidney--phosphate concrement associated with uric urease producing infection.
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PMID:[Prediction of changes in chemical form of urolithiasis]. 2181 53

The effects of long-term (29 years) fertilization on local agro-ecosystems in the Loess Plateau of northwest China, containing a single or combinations of inorganic (Nitrogen, N; Phosphate, P) and organic (Mature, M Straw, S) fertilizer, including N, NP, SNP, M, MNP, and a control. The soil enzymes, including dehydrogenase, urease, alkaline phosphatase, invertase and glomalin, were investigated in three physiological stages (Jointing, Dough, and Maturity) of wheat growth at three depths of the soil profile (0-15, 16-30, 31-45 cm). We found that the application of farmyard manure and straw produced the highest values of soil enzymatic activity, especially a balanced applied treatment of MNP. Enzymatic activity was lowest in the control. Values were generally highest at dough, followed by the jointing and maturity stages, and declined with soil profile depth. The activities of the enzymes investigated here are significantly correlated with each other and are correlated with soil nutrients, in particular with soil organic carbon. Our results suggest that a balanced application of fertilizer nutrients and organic manure (especially those containing P) has positive effects on multiple soil chemical parameters, which in turn enhances enzyme activity. We emphasize the role of organic manure in maintaining soil organic matter and promoting biological activity, as its application can result in a substantial increase in agricultural production and can be sustainable for many years.
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PMID:Long-term effects of fertilizer on soil enzymatic activity of wheat field soil in Loess Plateau, China. 2513 79


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