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PfATP6 : ウィキペディア英語版
PfATP6
PfATP6, also known as PfSERCA or PfATPase6, is a calcium ATPase gene encoded by the malaria parasite ''Plasmodium falciparum''. The protein is thought to be a P-type ATPase involved in calcium ion transport. Mutations in this gene may affect resistance to artemisinin antimalarial medication.
==Resistance to artemisinin antimalarials==
It has been suggested that PfATP6 is a target of artemisinin antimalarials, and also that a single amino acid mutation in the enzyme can mediate resistance to this important group of compounds. Findings supporting PfATP6 as the target have subsequently been confirmed in an independent series of experiments that use yeast expressing this Ca2+ ATPase. Artemisinins selectively and reproducibly inhibit the yeast growth by their actions on PfATP6, as well as providing information on the effects of mutations in PfATP6 on drug sensitivity. In French Guiana and Senegal reduced sensitivity to artemisinins have been associated with single nucleotide polymorphisms in PfATP6. Predictions made by laboratory models that mutations in PfATP6 might be associated with artemisinin selection have been independently validated by the discovery of a predicted single nucleotide polymorphism in Tanzania.〔Jaffu Chilongola, Arnold Ndaro, Hipolite Tarimo, et al., ()"Occurrence of pfatpase6 Single Nucleotide Polymorphisms Associated with Artemisinin Resistance among Field Isolates of Plasmodium falciparum in North-Eastern Tanzania," Malaria Research and Treatment, vol. 2015, Article ID 279028, 7 pages, 2015. 〕This is the first evidence in field isolates, and confirms the prescience of laboratory models that have been developed to study interactions of artemisinins with PfATP6 as well as supporting epidemiological studies to monitor changes in the frequency of single nucleotide polymorphisms in this target.
The mammalian Ca++ ATPase SERCA1a was also inhibited by artemisinins in coupled enzyme assays, and mutations in either SERCA1a or pfATP6 modulate their sensitivity to artemisinin.
Anomalously, if either pfATP6 or SERCA1a are detergent solubilised, they do not show sensitivity to artemisinins.

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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