Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:6.3.4.6 (urease)
 7,490 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Struvite calculi can be produced in the bladder of Sprague-Dawley male rats after injection of ureaplasmas into the renal medulla. Calculi appear 3 to 6 days after ureaplasma injection. We have studied the inhibitory effect of flurofamide, a potent inhibitor of Ureaplasma urealyticum urease, and doxycycline, on the formation of bladder stones. Flurofamide given orally in five doses (total 125 mg) over 3 days and doxycycline in seven doses (total 20 mg) over 4 days partially prevented stone formation only when given at the time of inoculation. Ureaplasmas disappeared rapidly from the urine. The inhibitory effect of flurofamide was higher than that of doxycycline. However, doxycycline seemed to be efficient when given for a long period (5 weeks).
 ...
PMID:Ureaplasma-urealyticum-induced bladder stones in rats and their prevention by flurofamide and doxycycline. 366 26

Flurofamide, a potent inhibitor of urease, at concentrations of 0.0007 to 0.001 mg/l inhibited the multiplication of three ureaplasma strains of human genital origin (one tetracycline-resistant) and two and three strains of marmoset genital and oral origin, respectively. However, a more than 1000-fold greater concentration of the drug was required to kill the organisms. Flurofamide did not inhibit the growth of arginine-hydrolysing or glucose-fermenting mycoplasmas, indicating its specificity for ureaplasmas. When it was given orally in a dose of 25 mg twice on one day and 25 mg on one further day to marmosets infected naturally with ureaplasmas in their throats, the organisms disappeared rapidly. The animals remained ureaplasma-free for 42 to 106 days, at which time they were successfully infected experimentally.
 ...
PMID:The inhibitory effect of flurofamide on ureaplasmas and their elimination from marmosets by its use. 644 Aug 84

Flurofamide (N-[diaminophosphinyl]-4-fluorobenzamide), a urease inhibitor, was a potent inhibitor of the growth of Ureaplasma urealyticum. As little as 10 microM flurofamide (2 micrograms/ml) prevented any growth, but U. urealyticum survived for about eight hours before colony counts become undetectable. Flurofamide was a specific inhibitor of U. urealyticum since it did not inhibit growth of four Mycoplasma species or Acholeplasma hippikon. Flurofamide was 1,000 times more active than acetohydroxamic acid and thus has promise as a chemotherapeutic agent and a biochemical tool.
 ...
PMID:Inhibition of the growth of Ureaplasma urealyticum by a new urease inhibitor, flurofamide. 667 52

Infectious meningitis and encephalitis is caused by invasion of circulating pathogens into the brain. It is unknown how the circulating pathogens dynamically interact with brain endothelium under shear stress, leading to invasion into the brain. Here, using intravital microscopy, we have shown that Cryptococcus neoformans, a yeast pathogen that causes meningoencephalitis, stops suddenly in mouse brain capillaries of a similar or smaller diameter than the organism, in the same manner and with the same kinetics as polystyrene microspheres, without rolling and tethering to the endothelial surface. Trapping of the yeast pathogen in the mouse brain was not affected by viability or known virulence factors. After stopping in the brain, C. neoformans was seen to cross the capillary wall in real time. In contrast to trapping, viability, but not replication, was essential for the organism to cross the brain microvasculature. Using a knockout strain of C. neoformans, we demonstrated that transmigration into the mouse brain is urease dependent. To determine whether this could be amenable to therapy, we used the urease inhibitor flurofamide. Flurofamide ameliorated infection of the mouse brain by reducing transmigration into the brain. Together, these results suggest that C. neoformans is mechanically trapped in the brain capillary, which may not be amenable to pharmacotherapy, but actively transmigrates to the brain parenchyma with contributions from urease, suggesting that a therapeutic strategy aimed at inhibiting this enzyme could help prevent meningitis and encephalitis caused by C. neoformans infection.
 ...
PMID:Real-time imaging of trapping and urease-dependent transmigration of Cryptococcus neoformans in mouse brain. 2042 19