Antimalarial drug discovery: Progress and approaches

JL Siqueira-Neto, KJ Wicht, K Chibale… - Nature Reviews Drug …, 2023 - nature.com
Recent antimalarial drug discovery has been a race to produce new medicines that
overcome emerging drug resistance, whilst considering safety and improving dosing …

Pantothenate and CoA biosynthesis in Apicomplexa and their promise as antiparasitic drug targets

LE de Vries, M Lunghi, A Krishnan, TWA Kooij… - PLoS …, 2021 - journals.plos.org
The Apicomplexa phylum comprises thousands of distinct intracellular parasite species,
including coccidians, haemosporidians, piroplasms, and cryptosporidia. These parasites are …

Potent acyl-CoA synthetase 10 inhibitors kill Plasmodium falciparum by disrupting triglyceride formation

S Bopp, CFA Pasaje, RL Summers… - Nature …, 2023 - nature.com
Identifying how small molecules act to kill malaria parasites can lead to new “chemically
validated” targets. By pressuring Plasmodium falciparum asexual blood stage parasites with …

1, 5, 7-Triazabicyclo [4.4. 0] dec-5-ene: an effective catalyst for amide formation by lactone aminolysis

CB Lan, K Auclair - The Journal of Organic Chemistry, 2023 - ACS Publications
The amide is one of the most prevalent functional groups throughout natural and engineered
chemical space. Among various methods of constructing amide bonds, lactone aminolysis …

A versatile Plasmodium falciparum reporter line expressing NanoLuc enables highly sensitive multi-stage drug assays

Y Miyazaki, MW Vos, FJA Geurten, P Bigeard… - Communications …, 2023 - nature.com
Transgenic luciferase-expressing Plasmodium falciparum parasites have been widely used
for the evaluation of anti-malarial compounds. Here, to screen for anti-malarial drugs …

Eliminating malaria transmission requires targeting immature and mature gametocytes through lipoidal uptake of antimalarials

M Naude, A van Heerden, J Reader… - Nature …, 2024 - nature.com
Novel antimalarial compounds targeting both the pathogenic and transmissible stages of the
human malaria parasite, Plasmodium falciparum, would greatly benefit malaria elimination …

Recent advances in measurement of metabolic clearance, metabolite profile and reaction phenotyping of low clearance compounds

L Di - Expert Opinion on Drug Discovery, 2023 - Taylor & Francis
Introduction Low metabolic clearance is usually a highly desirable property of drug
candidates in order to reduce dose and dosing frequency. However, measurement of low …

New targets for antimalarial drug discovery

F Guerra, EA Winzeler - Current opinion in microbiology, 2022 - Elsevier
Highlights•Many antimalarial drug targets discovered using reverse chemical genetic
methods are druggable in other species.•tRNA synthetases seem to be one of the most …

Recent metabolomic developments for antimalarial drug discovery

L Mamede, F Fall, M Schoumacher, A Ledoux… - Parasitology …, 2022 - Springer
Malaria is a parasitic disease that remains a global health issue, responsible for a significant
death and morbidity toll. Various factors have impacted the use and delayed the …

Molecular mechanisms of mitochondria-mediated ferroptosis: a potential target for antimalarial interventions

AG Adegboro, IS Afolabi - Frontiers in Cell and Developmental …, 2024 - frontiersin.org
Ferroptosis is an iron-dependent form of regulated cell death characterized by glutathione
(GSH) depletion, glutathione peroxidase 4 (GPX4) inactivation, and the build-up of lipotoxic …