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Abstract Title:

The anthraquinone emodin inhibits the non-exported FIKK kinase from Plasmodium falciparum.

Abstract Source:

Bioorg Chem. 2017 Sep 18 ;75:217-223. Epub 2017 Sep 18. PMID: 28987877

Abstract Author(s):

Benjamin C Lin, Darcy R Harris, Lucy M D Kirkman, Astrid M Perez, Yiwen Qian, Janse T Schermerhorn, Min Y Hong, Dennis S Winston, Lingyin Xu, Alexander M Lieber, Matthew Hamilton, Gabriel S Brandt

Article Affiliation:

Benjamin C Lin

Abstract:

The FIKK family of kinases is unique to parasites of the Apicomplexan order, which includes all malaria parasites. Plasmodium falciparum, the most virulent form of human malaria, has a family of 19 FIKK kinases, most of which are exported into the host red blood cell during malaria infection. Here, we confirm that FIKK 8 is a non-exported member of the FIKK kinase family. Through expression and purification of the recombinant kinase domain, we establish that emodin is a relatively high-affinity (IC50=2μM) inhibitor of PfFk8. Closely related anthraquinones do not inhibit PfFk8, suggesting that the particular substitution pattern of emodin is critical to the inhibitory pharmacophore. This first report of a P. falciparum FIKK kinase inhibitor lays the groundwork for developing specific inhibitors of the various members of the FIKK kinase family in order to probe their physiological function.

Study Type : In Vitro Study
Additional Links
Pharmacological Actions : Antimalarials : CK(41) : AC(24)

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