A chemical rescue screen identifies a Plasmodium falciparum apicoplast inhibitor targeting MEP isoprenoid precursor biosynthesis

W Wu, Z Herrera, D Ebert, K Baska… - Antimicrobial agents …, 2015 - Am Soc Microbiol
The apicoplast is an essential plastid organelle found in Plasmodium parasites which
contains several clinically validated antimalarial-drug targets. A chemical rescue screen …

[HTML][HTML] Chemical Rescue of Malaria Parasites Lacking an Apicoplast Defines Organelle Function in Blood-Stage Plasmodium falciparum

E Yeh, JL DeRisi - PLoS biology, 2011 - journals.plos.org
Plasmodium spp parasites harbor an unusual plastid organelle called the apicoplast. Due to
its prokaryotic origin and essential function, the apicoplast is a key target for development of …

Determination of the active stereoisomer of the MEP pathway-targeting antimalarial agent MMV008138, and initial structure–activity studies

ZK Yao, PM Krai, EF Merino, ME Simpson… - Bioorganic & medicinal …, 2015 - Elsevier
Compounds that target isoprenoid biosynthesis in Plasmodium falciparum could be a
welcome addition to malaria chemotherapy, since the methylerythritol phosphate (MEP) …

Plasmodium IspD (2-C-Methyl-d-erythritol 4-Phosphate Cytidyltransferase), an Essential and Druggable Antimalarial Target

LS Imlay, CM Armstrong, MC Masters, T Li… - ACS Infectious …, 2015 - ACS Publications
As resistance to current therapies spreads, novel antimalarials are urgently needed. In this
work, we examine the potential for therapeutic intervention via the targeting of Plasmodium …

[HTML][HTML] The interdependence of isoprenoid synthesis and apicoplast biogenesis in malaria parasites

M Okada, PA Sigala - PLoS Pathogens, 2023 - journals.plos.org
Isoprenoid precursor synthesis is an ancient and fundamental function of plastid organelles
and a critical metabolic activity of the apicoplast in Plasmodium malaria parasites [–]. Over …

[HTML][HTML] New Insight into Isoprenoids Biosynthesis Process and Future Prospects for Drug Designing in Plasmodium

GS Saggu, ZR Pala, S Garg, V Saxena - Frontiers in Microbiology, 2016 - frontiersin.org
The MEP (Methyl Erythritol Phosphate) isoprenoids biosynthesis pathway is an attractive
drug target to combat malaria, due to its uniqueness and indispensability for the parasite. It …

Validation of putative apicoplast-targeting drugs using a chemical supplementation assay in cultured human malaria parasites

T Uddin, GI McFadden… - Antimicrobial agents and …, 2018 - Am Soc Microbiol
Malaria parasites contain a relict plastid, the apicoplast, which is considered an excellent
drug target due to its bacterial-like ancestry. Numerous parasiticidals have been proposed to …

[HTML][HTML] MEPicides: potent antimalarial prodrugs targeting isoprenoid biosynthesis

RL Edwards, RC Brothers, X Wang, MI Maron… - Scientific reports, 2017 - nature.com
The emergence of Plasmodium falciparum resistant to frontline therapeutics has prompted
efforts to identify and validate agents with novel mechanisms of action. MEPicides represent …

[HTML][HTML] Delayed death in the malaria parasite Plasmodium falciparum is caused by disruption of prenylation-dependent intracellular trafficking

K Kennedy, SA Cobbold, E Hanssen, J Birnbaum… - PLoS …, 2019 - journals.plos.org
Apicomplexan parasites possess a plastid organelle called the apicoplast. Inhibitors that
selectively target apicoplast housekeeping functions, including DNA replication and protein …

[HTML][HTML] A mevalonate bypass system facilitates elucidation of plastid biology in malaria parasites

RP Swift, K Rajaram, HB Liu, A Dziedzic… - PLoS …, 2020 - journals.plos.org
Malaria parasites rely on a plastid organelle for survival during the blood stages of infection.
However, the entire organelle is dispensable as long as the isoprenoid precursor …