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Review
. 2011 Jan 18;50(2):163-71.
doi: 10.1021/bi101638n. Epub 2010 Dec 22.

PfCRT-mediated drug transport in malarial parasites

Paul D Roepe  1
Affiliations
Review

PfCRT-mediated drug transport in malarial parasites

Paul D Roepe. Biochemistry. .

Abstract

A wide range of drug transport studies using intact infected red blood cells, isolated malarial parasites, heterologous expression systems, and purified protein, combined with elegant genetic experiments, have suggested that chloroquine transport by the Plasmodium falciparum chloroquine resistance transporter (PfCRT) is a key aspect of the molecular mechanism of quinoline antimalarial drug resistance. However, many questions remain. This short review summarizes data that have led to drug channel versus drug pump hypotheses for PfCRT and suggests ways in which recent contrasting interpretations might be reconciled.

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Figures

Figure
Figure
Schematic of PfCRT protein generated using TMRPres2D (http://bioinformatics.biol.uoa.gr/TMRPres2D/index.jsp). Vertical arrow indicates the covalent attachment site of the terminal domain of a CQ photoaffinity probe [62]. Dashed boxes (horizontal arrows) denote the proposed binding site of the chloroquine quinolinal ring system, based on photolabelling data and mass spectrometry (see [62]).
See this image and copyright information in PMC

References

    1. Fidock DA, Nomura T, Talley AK, Cooper RA, Dzekunov SA, Ferdig MT, Ursos LM, Sidhu AB, Naude B, Deitsch KW, Su XZ, Wootton JC, Roepe PD, Wellems TE. Mutations in the P. falciparum digestive vacuole transmembrane protein PfCRT and evidence for their role in chloroquine resistance. Molecular Cell. 2000;6:861–871. - PMC - PubMed
    1. Roepe PD. Molecular and physiologic basis of quinoline drug resistance in Plasmodium falciparum malaria. Future Microbiol. 2009;4:441–455. - PMC - PubMed
    1. Hayton K, Su XZ. Drug resistance and genetic mapping in Plasmodium falciparum. Curr Genet. 2008;54(5):223–239. - PubMed
    1. Plowe CV. The evolution of drug-resistant malaria. Trans R Soc Trop Med Hyg. 2009;103:S11–14. - PMC - PubMed
    1. Jiang H, Patel JJ, Yi M, Mu J, Ding J, Stephens R, Cooper RA, Ferdig MT, Su XZ. Genome-wide compensatory changes accompany drug- selected mutations in the Plasmodium falciparum crt gene. PLoS One. 2008;3:e2484. - PMC - PubMed

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