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


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(90) : AC(53)

Print Options

Key Research Topics

Sayer Ji
Founder of GreenMedInfo.com

Subscribe to our informative Newsletter & get Nature's Evidence-Based Pharmacy

Our newsletter serves 500,000 with essential news, research & healthy tips, daily.

Download Now

500+ pages of Natural Medicine Alternatives and Information.

This website is for information purposes only. By providing the information contained herein we are not diagnosing, treating, curing, mitigating, or preventing any type of disease or medical condition. Before beginning any type of natural, integrative or conventional treatment regimen, it is advisable to seek the advice of a licensed healthcare professional.

© Copyright 2008-2022 GreenMedInfo.com, Journal Articles copyright of original owners, MeSH copyright NLM.