Department of Medicine, Yale University School of Medicine, New Haven, Connecticut 06520, USA.
J Biol Chem. 2013 Jul 12;288(28):20558-67. doi: 10.1074/jbc.M113.482992. Epub 2013 May 31.
The human malaria parasite Plasmodium falciparum is absolutely dependent on the acquisition of host pantothenate for its development within human erythrocytes. Although the biochemical properties of this transport have been characterized, the molecular identity of the parasite-encoded pantothenate transporter remains unknown. Here we report the identification and functional characterization of the first protozoan pantothenate transporter, PfPAT, from P. falciparum. We show using cell biological, biochemical, and genetic analyses that this transporter is localized to the parasite plasma membrane and plays an essential role in parasite intraerythrocytic development. We have targeted PfPAT to the yeast plasma membrane and showed that the transporter complements the growth defect of the yeast fen2Δ pantothenate transporter-deficient mutant and mediates the entry of the fungicide drug, fenpropimorph. Our studies in P. falciparum revealed that fenpropimorph inhibits the intraerythrocytic development of both chloroquine- and pyrimethamine-resistant P. falciparum strains with potency equal or better than that of currently available pantothenate analogs. The essential function of PfPAT and its ability to deliver both pantothenate and fenpropimorph makes it an attractive target for the development and delivery of new classes of antimalarial drugs.
人类疟疾寄生虫疟原虫对其在人类红细胞内的发育绝对依赖于宿主泛酸的获取。尽管这种运输的生化特性已经得到了描述,但寄生虫编码的泛酸转运蛋白的分子身份仍然未知。在这里,我们报告了疟原虫 PfPAT 的鉴定和功能特征,PfPAT 是第一个原生动物泛酸转运蛋白。我们通过细胞生物学、生物化学和遗传分析表明,这种转运蛋白定位于寄生虫质膜,在寄生虫内红细胞发育中起着至关重要的作用。我们已经将 PfPAT 靶向酵母质膜,并表明该转运蛋白可以弥补酵母 fen2Δ 泛酸转运蛋白缺陷突变体的生长缺陷,并介导杀真菌剂药物苯丙嘧啶的进入。我们在疟原虫中的研究表明,苯丙嘧啶抑制氯喹和乙胺嘧啶耐药疟原虫株的红细胞内发育,其效力与现有泛酸盐类似物相当或更好。PfPAT 的必需功能及其能够输送泛酸和苯丙嘧啶的能力使其成为开发和输送新型抗疟药物的有吸引力的靶标。