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Anticancer Drugs, Ionophoric Peptides, and Steroids as Substrates of the Yeast Multidrug Transporter Pdr5p*
TLDR
It is shown that in spite of little sequence homology, and inverted topology in respect to that of mammalian P-glycoproteins, Pdr5p shares with them common substrates, and the experimental system opens new possibilities for the analysis of structure-function relationship of multidrug transporter substrates and inhibitors. Expand
The pleitropic drug ABC transporters from Saccharomyces cerevisiae.
TLDR
Three plasma membrane multidrug exporters are studied in detail and the substrate specificity of Pdr5p, Snq2p and Yor1p are largely, but not totally, overlapping as shown by screening the growth inhibition by 349 toxic compounds of combinatorial deletants of these three ABC genes. Expand
In vivo characterization of the drug resistance profile of the major ABC transporters and other components of the yeast pleiotropic drug resistance network.
TLDR
Identification of compounds showing Pdr1p, Pdr3p-dependent, but Pdr5p-, Snq2p-, and Yor1p-independent toxicity suggests the involvement of new drug resistance genes and is a first step toward their identification. Expand
Solubilization and characterization of the overexpressed PDR5 multidrug resistance nucleotide triphosphatase of yeast.
TLDR
Many of these properties liken PDR5 to the purified mammalian P-glycoprotein responsible for multidrug resistance, which is sensitive to low concentrations of vanadate, of oligomycin, and of a variety of hydrophobic compounds. Expand
Compensatory activation of the multidrug transporters Pdr5p, Snq2p, and Yor1p by Pdr1p in Saccharomyces cerevisiae
TLDR
Growth resistance to specific Pdr5p substrates rose upon disruption of the YOR1 or SNQ2 coding region and was accompanied by increased efflux, and resistance to Yor1p‐ and Snq2p‐specific substrates increased upon deletion of PDR5. Expand
Drug resistance mechanisms and their regulation in non-albicans Candida species.
TLDR
Findings concerning underlying mechanisms associated with elevated drug resistance suggest a link to cell wall and plasma membrane metabolism in non-albicans Candida species. Expand
Functional dissection of Pdr1p, a regulator of multidrug resistance in Saccharomyces cerevisiae
TLDR
A mini-Pdr1p consisting of only the DNA-binding and the activation domains strongly up-regulates the expression of the major target genes PDR5, SNQ2 and YOR1, resulting in enhanced multidrug resistance. Expand
Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT6 receptor antagonists. Design, synthesis and biological evaluation.
TLDR
A novel class of multifunctional ligands with compound 12 as the best derivative in a series represents an excellent starting point for the further development of an effective treatment for AD. Expand
Differential Regulation of Ceramide Synthase Components LAC1 and LAG1 in Saccharomyces cerevisiae
TLDR
Detailed analyses of the LAC1 promoter demonstrated that transcription of this gene is inhibited by the presence of the transcription factor Cbf1p and the anaerobic repressor Rox1p, demonstrating extensive coordinate control of sphingolipid biosynthesis and multidrug resistance in yeast. Expand
Fungal ABC transporter-associated activity of isoflavonoids from the root extract of Dalea formosa.
TLDR
The results demonstrate that multiple crude extract compounds are differentially affected by efflux-mediated resistance and are collectively responsible for the observed bioactivity. Expand
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