Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.

@article{Gorka2013QuinolineDI,
  title={Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.},
  author={Alexander P. Gorka and Angel C de Dios and Paul D Roepe},
  journal={Journal of medicinal chemistry},
  year={2013},
  volume={56 13},
  pages={5231-46}
}
Historically, the most successful molecular target for antimalarial drugs has been heme biomineralization within the malarial parasite digestive vacuole. Heme released from catabolized host red blood cell hemoglobin is toxic, so malarial parasites crystallize heme to nontoxic hemozoin. For years it has been accepted that a number of effective quinoline antimalarial drugs (e.g., chloroquine, quinine, amodiaquine) function by preventing hemozoin crystallization. However, recent studies over the… CONTINUE READING
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