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In Vitro Activities of Posaconazole, Fluconazole, Itraconazole, Voriconazole, and Amphotericin B against a Large Collection of Clinically Important Molds and Yeasts
Posaconazole exhibited potent antifungal activity against a wide variety of clinically important fungal pathogens and was frequently more active than other azoles and amphotericin B.
Three-Dimensional Models of Wild-Type and Mutated Forms of Cytochrome P450 14α-Sterol Demethylases from Aspergillus fumigatus and Candida albicans Provide Insights into Posaconazole Binding
ABSTRACT The cytochrome P450 sterol 14α-demethylase enzyme (CYP51) is the target of azole antifungals. Azoles block ergosterol synthesis, and thereby fungal growth, by binding in the active-site
Mutations in Aspergillus fumigatus Resulting in Reduced Susceptibility to Posaconazole Appear To Be Restricted to a Single Amino Acid in the Cytochrome P450 14α-Demethylase
The transformants exhibited reductions in susceptibility to POS comparable to those exhibited by the original mutants, confirming that point mutations in the cyp51A gene in A. fumigatus can confer reduced susceptibility to Posaconazole.
Application of Real-Time Quantitative PCR to Molecular Analysis of Candida albicans Strains Exhibiting Reduced Susceptibility to Azoles
Despite both the increases in pump expression and the ERG11 mutations, only one of the patient isolates exhibited a large decrease in posaconazole susceptibility.
A novel site of antibiotic action in the ribosome: Interaction of evernimicin with the large ribosomal subunit
RNA probing demonstrated that the drug protects a specific set of nucleotides in the loops of hairpins 89 and 91 of 23S rRNA in bacterial and archaeal ribosomes in Evernimicin-resistant mutants of Halobacterium halobium.
EmtA, a rRNA methyltransferase conferring high‐level evernimicin resistance
RNA footprinting revealed that G2470 is located within the evernimicin‐binding site on the ribosome, thus providing an explanation for the reduced binding of the drug to methylated ribosomes.
Comparative in vitro activities of posaconazole, voriconazole, itraconazole, and amphotericin B against Aspergillus and Rhizopus, and synergy testing for Rhizopus.
In studies with R. oryzae isolates, posaconazoles was found to be the most potent drug followed by itraconazole and amphotericin B, in order of decreasing activity, and in studies with Aspergillus spp.
Anaerobic regulation of the Escherichia coli dmsABC operon requires the molybdate‐responsive regulator ModE
This study provides the first example in which ModE affects gene regulation in concert with another transcription factor, and identifies a putative integration host factor (IHF) binding site in the intervening sequence, and in vitro studies confirmed that IHF bound this site with high affinity.
Changes in susceptibility to posaconazole in clinical isolates of Candida albicans.
Multiple mutations in ERG11 are required to confer decreased susceptibility to posaconazole in Candida albicans clinical isolates.
Characterization of the ModE DNA‐binding sites in the control regions of modABCD and moaABCDE of Escherichia coli
It is demonstrated that ModE acts both as a repressor and activator of the mod and moa operons, respectively, depending on the properties of the binding site.