Crystal Structure of the Apo and the ADP-Bound Form of Choline Kinase from Plasmodium falciparum

Crystals

Emilio Parisini¹  Archimede Torretta¹  LuisaCarlota Lopez-Cara² 

[1] Center for Nano Science and Technology @PoliMi, Istituto Italiano di Tecnologia, Via Pascoli 70/3, 20133 Milano, Italy;Department of Pharmaceutical and Organic Chemistry, Faculty of Pharmacy, Campus of Cartuja, 18071 Granada, Spain;

关键词: choline kinase;    Plasmodium falciparum;    malaria;    ADP;    crystal structure;   

DOI  :  10.3390/cryst10070613

来源: DOAJ

【 摘 要 】

Among the malaria-causing parasites, the deadliest is Plasmodium falciparum, which accounts for the majority of the fatalities. As the infection progresses inside erythrocytes, major cellular and metabolic changes take place. For its own growth, the parasite relies on the accumulation of phospholipids, which are essential for membrane synthesis. Within the Kennedy pathway, the P. falciparum choline kinase (PfChoK) has a central role in the biosynthesis of phosphatidylcholine and its selective inhibition leads to the parasite arrest and eradication. Here, we report the crystal structure of the apo and the ADP-bound form of choline kinase from Plasmodium falciparum at 2.0 and 2.2 Å resolution, respectively. These new structural data will facilitate the implementation of effective structure-based drug development strategies against PfChoK in the fight against malaria.

【 授权许可】

Unknown