[HTML][HTML] Current and emerging target identification methods for novel antimalarials

MP Challis, SM Devine, DJ Creek - International Journal for Parasitology …, 2022 - Elsevier
New antimalarial compounds with novel mechanisms of action are urgently needed to
combat the recent rise in antimalarial drug resistance. Phenotypic high-throughput screens …

Redox-based strategies against infections by eukaryotic pathogens

C Vallières, MP Golinelli-Cohen, O Guittet, M Lepoivre… - Genes, 2023 - mdpi.com
Redox homeostasis is an equilibrium between reducing and oxidizing reactions within cells.
It is an essential, dynamic process, which allows proper cellular reactions and regulates …

Dietary aflatoxin B1 and antimalarial—a lumefantrine/artesunate—therapy perturbs male rat reproductive function via pro-inflammatory and oxidative mechanisms

SE Owumi, AO Umez, U Arunsi, CE Irozuru - Scientific Reports, 2023 - nature.com
We investigated the impact of Coartem™(COA) and aflatoxin B1 (AFB1) on rats'
hypothalamus, epididymis, and testis. Male rats were randomly grouped (n= 5 rats) and …

Access to Artemisinin–Triazole Antimalarials via Organo-Click Reaction: High In Vitro/In Vivo Activity against Multi-Drug-Resistant Malaria Parasites

L Herrmann, M Leidenberger, HC Quadros, BW Grau… - JACS Au, 2024 - ACS Publications
Malaria is one of the most widespread diseases worldwide. Besides a growing number of
people potentially threatened by malaria, the consistent emergence of resistance against …

[HTML][HTML] Chemoproteomics validates selective targeting of Plasmodium M1 alanyl aminopeptidase as an antimalarial strategy

D Creek, C Giannangelo, M Challis, G Siddiqui… - eLife, 2024 - elifesciences.org
New antimalarial drug candidates that act via novel mechanisms are urgently needed to
combat malaria drug resistance. Here, we describe the multi-omic chemical validation of …

Lewis acids and heteropoly acids in the synthesis of organic peroxides

IA Yaremenko, PS Radulov, YY Belyakova… - Pharmaceuticals, 2022 - mdpi.com
Organic peroxides are an important class of compounds for organic synthesis,
pharmacological chemistry, materials science, and the polymer industry. Here, for the first …

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 …

Bibliometric analysis of antimalarial drug resistance

J Zhang, M Shahbaz, M Ijaz, H Zhang - Frontiers in Cellular and …, 2024 - frontiersin.org
Background Malaria has always been a serious infectious disease prevalent in the world.
Antimalarial drugs such as chloroquine and artemisinin have been the main compounds …

Artefenomel regioisomer RLA-3107 is a promising lead for the discovery of next-generation endoperoxide antimalarials

BR Blank, J Gut, PJ Rosenthal… - ACS Medicinal Chemistry …, 2023 - ACS Publications
Clinical development of the antimalarial artefenomel was recently halted due to formulation
challenges stemming from the drug's lipophilicity and low aqueous solubility. The symmetry …

Chemoproteomics validates selective targeting of Plasmodium M1 alanyl aminopeptidase as an antimalarial strategy

C Giannangelo, MP Challis, G Siddiqui, R Edgar… - Elife, 2024 - elifesciences.org
New antimalarial drug candidates that act via novel mechanisms are urgently needed to
combat malaria drug resistance. Here, we describe the multi-omic chemical validation of …