Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.6.1.3 (ATPase)
 65,361 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Staphylococcus aureus can be protected by unsaturated unesterified fatty acids against the growth inhibitory effects of miconazole and ketoconazole observed at concentrations greater than 10(-6) M and greater than 10(-5) M, respectively. Miconazole's fungicidal activity is partly antagonized by oleic acid. However, the effect of ketoconazole on the viability of Candida albicans was not affected by this fatty acid. Cytochrome oxidase and ATPase activities are more sensitive to miconazole (10(-5) M) than to ketoconazole (greater than 10(-4) M) and also liposomes are more susceptible to lysis induced by miconazole. Using differential scanning calorimetry it is shown that high concentrations of miconazole shift the lipid transition temperature of multilamellar vesicles to lower values without affecting the enthalpy of melting. Ketoconazole induces a broadening of the main transition peak only. It is suggested that miconazole changes the lipid organization without binding to the lipids, whereas ketoconazole is localized in the multilayer without having an important direct effect on the lipid organization. The results indicate that miconazole, and to a lesser extent ketoconazole, at doses that can be reached by topical application only, interfere with a third target (the two others are ergosterol synthesis and fatty acid elongation plus desaturation). It is hypothesized that the induced change in lipid organization may play some role in miconazole's topical antibacterial and fungicidal activity, whereas it does not seem to play a significant role in ketoconazole's activities.
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PMID:The interaction of miconazole and ketoconazole with lipids. 629 39

In this report, we study Ca2+ transport in permeabilized Candida parapsilosis spheroplasts prepared by a new technique using lyticase. An intracellular non-mitochondrial Ca2+ uptake pathway, insensitive to orthovanadate and sensitive to the V-H(+)-ATPase inhibitor bafilomycin A(1), nigericin and carbonyl cyanide p-trifluoromethoxyphenylhydrazone was characterized. Acidification of the compartment in which Ca2+ accumulated was followed using the fluorescent dye acridine orange. Acidification was stimulated by the Ca2+ chelator EGTA and inhibited by Ca2+. These results, when added to the observation that Ca2+ induces alkalization of a cellular compartment, provide evidence for the presence of a Ca2+/nH(+) antiporter in the acid compartment membrane. Interestingly, like in acidocalcisomes of trypanosomatids, the antioxidant 3,5-dibutyl-4-hydroxytoluene inhibits the V-H(+)-ATPase. In addition, the antifungal agent ketoconazole promoted a fast alkalization of the acidic compartment. Ketoconazole effects were dose-dependent and occurred in a concentration range close to that attained in the plasma of patients treated with this drug.
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PMID:Ca(2+) transport into an intracellular acidic compartment of Candida parapsilosis. 1143 31