Author(s): Uhlemann AC, Cameron A, EcksteinLudwig U, Fischbarg J, Iserovich P,
Abstract Share this page
Abstract Artemisinins are the most important class of antimalarial drugs. They specifically inhibit PfATP6, a SERCA-type ATPase of Plasmodium falciparum. Here we show that a single amino acid in transmembrane segment 3 of SERCAs can determine susceptibility to artemisinin. An L263E replacement of a malarial by a mammalian residue abolishes inhibition by artemisinins. Introducing residues found in other Plasmodium spp. also modulates artemisinin sensitivity, suggesting that artemisinins interact with the thapsigargin-binding cleft of susceptible SERCAs.
This article was published in Nat Struct Mol Biol
and referenced in Journal of Addiction Research & Therapy