# name
Plasmodium falciparum Choline Kinase Inhibition Leads to a Major
                Decrease in Phosphatidylethanolamine Causing Parasite Death

# metadata.dc.description.abstract[].value
Malaria is a life-threatening disease caused by different
                species of the protozoan parasite Plasmodium, with P. falciparum
                being the deadliest. Increasing parasitic resistance to existing
                antimalarials makes the necessity of novel avenues to treat this
                disease an urgent priority. The enzymes responsible for the
                synthesis of phosphatidylcholine and phosphatidylethanolamine
                are attractive drug targets to treat malaria as their selective
                inhibition leads to an arrest of the parasite's growth and cures
                malaria in a mouse model. We present here a detailed study that
                reveals a mode of action for two P. falciparum choline kinase
                inhibitors both in vitro and in vivo. The compounds present
                distinct binding modes to the choline/ethanolamine-binding site
                of P. falciparum choline kinase, reflecting different types of
                inhibition. Strikingly, these compounds primarily inhibit the
                ethanolamine kinase activity of the P. falciparum choline
                kinase, leading to a severe decrease in the
                phosphatidylethanolamine levels within P. falciparum, which
                explains the resulting growth phenotype and the parasites death.
                These studies provide an understanding of the mode of action,
                and act as a springboard for continued antimalarial development
                efforts selectively targeting P. falciparum choline kinase.

# metadata.dc.relation.isformatof[].value
Reproducció del document publicat a:
                http://dx.doi.org/10.1038/srep33189

# metadata.dc.relation.ispartof[].value
Scientific Reports, 2016, vol. 6, num. 33189

# metadata.dc.source[].value
Articles publicats en revistes (ISGlobal)

# metadata.dc.title[].value
Plasmodium falciparum Choline Kinase Inhibition Leads to a Major
                Decrease in Phosphatidylethanolamine Causing Parasite Death