Chloroquine Transport in Plasmodium falciparum. 2. Analysis of PfCRT-Mediated Drug Transport Using Proteoliposomes and a Fluorescent Chloroquine Probe
In: Biochemistry, Jg. 48 (2009-09-16), S. 9482-9491
Online
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Zugriff:
Mutations in the PfCRT protein cause chloroquine resistance (CQR), and earlier studies from our laboratory using plasma membrane inside-out vesicles (ISOV) prepared from yeast expressing recombinant PfCRT [Zhang, H., et al. (2004) Biochemistry 43, 8290−8296] suggested that the putative transporter mediates downhill facilitated diffusion of charged chloroquine (CQ). However, more recent experiments with a fluorescent CQ probe (NBD-CQ) presented in the accompanying paper (DOI 10.1021/bi901034r) indicated that the CQR phenotype in live parasites is associated with a reduced rate of ATP-dependent CQ uptake into the digestive vacuole (DV). An altered rate constant for uptake has multiple interpretations. To further investigate this phenomenon, PfCRT proteins found in chloroquine-sensitive (CQS) and CQR strains of Plasmodium falciparum were purified from yeast engineered to express “yeast optimized” pfcrt genes, reconstituted into proteoliposomes (PL), and efflux of NBD-CQ was measured from these PL. A membrane...
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Chloroquine Transport in Plasmodium falciparum. 2. Analysis of PfCRT-Mediated Drug Transport Using Proteoliposomes and a Fluorescent Chloroquine Probe
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Autor/in / Beteiligte Person: | Paguio, Michelle F. ; Roepe, Paul D. ; Cabrera, Mynthia |
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Zeitschrift: | Biochemistry, Jg. 48 (2009-09-16), S. 9482-9491 |
Veröffentlichung: | American Chemical Society (ACS), 2009 |
Medientyp: | unknown |
ISSN: | 1520-4995 (print) ; 0006-2960 (print) |
DOI: | 10.1021/bi901035j |
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