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Purified Plasmodium falciparum multi-drug resistance protein (PfMDR 1) binds a high affinity chloroquine analogue

Authors
Journal
Molecular and Biochemical Parasitology
0166-6851
Publisher
Elsevier
Volume
173
Issue
2
Identifiers
DOI: 10.1016/j.molbiopara.2010.05.012
Keywords
  • Photolabelling
  • Quinoline
  • Abc Transporter
  • Mefloquine
  • Quinine
Disciplines
  • Biology

Abstract

Abstract We utilize the recent successful overexpression of recombinant Plasmodium falciparum multi-drug resistance transporter, purification and reconstitution of the protein, and a novel high affinity chloroquine analogue to probe hypothesized interaction between the transporter and quinoline drugs. Results suggest that PfMDR1 binding sites for chloroquine, mefloquine, and quinine overlap, that P. falciparum chloroquine resistance transporter has intrinsically higher affinity for chloroquine relative to P. falciparum multi-drug resistance transporter, and that there is an isoform specific competition between the two transporters for binding of quinoline antimalarial drugs.

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