Bernhard Nocht Institute for Tropical Medicine, Bernhard Nocht Str. 74, 20359 Hamburg, Germany.
Department of Molecular Biology, Radboud University, Geert Grooteplein 26-28, 6525 GA Nijmegen, Netherlands.
Science. 2020 Jan 3;367(6473):51-59. doi: 10.1126/science.aax4735.
Artemisinin and its derivatives (ARTs) are the frontline drugs against malaria, but resistance is jeopardizing their effectiveness. ART resistance is mediated by mutations in the parasite's Kelch13 protein, but Kelch13 function and its role in resistance remain unclear. In this study, we identified proteins located at a Kelch13-defined compartment. Inactivation of eight of these proteins, including Kelch13, rendered parasites resistant to ART, revealing a pathway critical for resistance. Functional analysis showed that these proteins are required for endocytosis of hemoglobin from the host cell. Parasites with inactivated Kelch13 or a resistance-conferring Kelch13 mutation displayed reduced hemoglobin endocytosis. ARTs are activated by degradation products of hemoglobin. Hence, reduced activity of Kelch13 and its interactors diminishes hemoglobin endocytosis and thereby ART activation, resulting in parasite resistance.
青蒿素及其衍生物(ARTs)是治疗疟疾的一线药物,但耐药性正威胁着它们的疗效。ART 耐药性是由寄生虫 Kelch13 蛋白的突变介导的,但 Kelch13 的功能及其在耐药性中的作用仍不清楚。在这项研究中,我们鉴定了位于 Kelch13 定义的隔室中的蛋白质。这 8 种蛋白质中的 8 种,包括 Kelch13,失活后使寄生虫对 ART 产生抗性,揭示了一条对耐药性至关重要的途径。功能分析表明,这些蛋白质是从宿主细胞内摄取血红蛋白所必需的。失活 Kelch13 或具有耐药性的 Kelch13 突变的寄生虫显示血红蛋白摄取减少。ARTs 通过血红蛋白降解产物激活。因此,Kelch13 及其相互作用蛋白活性降低会减少血红蛋白摄取,从而降低 ART 激活,导致寄生虫耐药。