The Human Chk1 Inhibitor CHIR-124 Shows Multistage Activity Against <i>Plasmodium falciparum</i> via Dual Inhibition of <i>Pf</i> Ark1 and Hemozoin Formation.

ABSTRACT: The high burden of malaria and growing resistance to frontline antimalarials demand new drugs with reduced propensities for generating resistance. An attractive approach to identifying chemical hits as starting points for antimalarial drug discovery involves the repositioning and chemical optimization of compounds used in other disease areas that are active against the human malaria parasite Plasmodium falciparum . Here we show that the human checkpoint kinase 1 (Chk1) inhibitor CHIR-124 is active in vitro against both drug-sensitive and drug-resistant asexual blood stage parasites and competitively binds to several Plasmodium kinases, including P. falciparum aurora-related kinase-1 ( Pf Ark1). The compound also shows moderate activity against both the li

SUBMITTER: Wicht KJ 

PROVIDER: S-EPMC12338603 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature