Department of Chemistry, Department of Biochemistry and Cellular and Molecular Biology, Georgetown University, Washington, DC 20057, United States.
Biochemistry. 2011 Jan 18;50(2):163-71. doi: 10.1021/bi101638n. Epub 2010 Dec 22.
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.
大量使用完整感染的红细胞、分离的疟原虫、异源表达系统和纯化蛋白的药物转运研究,结合巧妙的遗传实验,表明恶性疟原虫氯喹耐药转运蛋白(PfCRT)对氯喹的转运是奎宁类抗疟药物耐药分子机制的一个关键方面。然而,仍有许多问题尚未解决。本文简要综述了导致 PfCRT 被认为是药物通道或药物泵的相关数据,并提出了最近出现的一些相互矛盾的解释如何得到协调。