Related Experiment Video
Updated: May 6, 2026
CRISPR/Cas9 Gene Editing to Make Conditional Mutants of Human Malaria Parasite P. falciparum
Published on: September 18, 2018
Repositioning a Human Kinase Platelet-Derived Growth Factor Receptor Alpha Type II Inhibitor for Malaria and
Mmakwena M Mmonwa1,2, Oluwatosin Audu1, Keletso Maepa3
1Holistic Drug Discovery and Development (H3D) Centre, Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
None:
A type II Platelet-Derived Growth Factor Receptor Alpha (PDGFRA) human kinase inhibitor GSK190937, with antiplasmodium activity against asexual blood stage parasites (PfNF54 IC50 = 0.22 μM) was identified from the Kinase Chemogenomics Set, a collection of narrow-spectrum human kinase inhibitors. Medicinal chemistry progression of the hit focused on improving potency, selectivity, and ADME properties, leading to compounds 20, 23, and 29 with improved microsomal metabolic stability and asexual blood stage antiplasmodium activity. Mechanism of action studies showed that this series inhibits hemozoin formation, killing late-stage trophozoites.
