Antimalarial drug resistance: linking Plasmodium falciparum parasite biology to the clinic

B Blasco, D Leroy, DA Fidock - Nature medicine, 2017 - nature.com
The global adoption of artemisinin-based combination therapies (ACTs) in the early 2000s
heralded a new era in effectively treating drug-resistant Plasmodium falciparum malaria …

Cryo-EM in drug discovery: achievements, limitations and prospects

JP Renaud, A Chari, C Ciferri, W Liu… - Nature reviews Drug …, 2018 - nature.com
Cryo-electron microscopy (cryo-EM) of non-crystalline single particles is a biophysical
technique that can be used to determine the structure of biological macromolecules and …

[HTML][HTML] Protein X-ray crystallography and drug discovery

L Maveyraud, L Mourey - Molecules, 2020 - mdpi.com
With the advent of structural biology in the drug discovery process, medicinal chemists
gained the opportunity to use detailed structural information in order to progress screening …

[HTML][HTML] Plasmodium falciparum resistance to artemisinin-based combination therapies

KE Ward, DA Fidock, JL Bridgford - Current opinion in microbiology, 2022 - Elsevier
Highlights•Mutant K13-mediated artemisinin resistance involves reduced hemoglobin
endocytosis.•Artemisinin partial resistance has emerged in Africa.•Novel PfCRT mutations …

[HTML][HTML] Targeting tumor hypoxia and mitochondrial metabolism with anti-parasitic drugs to improve radiation response in high-grade gliomas

F Mudassar, H Shen, G O'Neill, E Hau - Journal of Experimental & Clinical …, 2020 - Springer
Abstract High-grade gliomas (HGGs), including glioblastoma and diffuse intrinsic pontine
glioma, are amongst the most fatal brain tumors. These tumors are associated with a dismal …

Identifying purine nucleoside phosphorylase as the target of quinine using cellular thermal shift assay

JM Dziekan, H Yu, D Chen, L Dai, G Wirjanata… - Science translational …, 2019 - science.org
Mechanisms of action (MoAs) have been elusive for most antimalarial drugs in clinical use.
Decreasing responsiveness to antimalarial treatments stresses the need for a better …

A Legionella toxin exhibits tRNA mimicry and glycosyl transferase activity to target the translation machinery and trigger a ribotoxic stress response

A Subramanian, L Wang, T Moss, M Voorhies… - Nature Cell …, 2023 - nature.com
A widespread strategy employed by pathogens to establish infection is to inhibit host-cell
protein synthesis. Legionella pneumophila, an intracellular bacterial pathogen and the …

Synthetic group A streptogramin antibiotics that overcome Vat resistance

Q Li, J Pellegrino, DJ Lee, AA Tran, HA Chaires… - Nature, 2020 - nature.com
Natural products serve as chemical blueprints for most antibiotics in clinical use. The
evolutionary process by which these molecules arise is inherently accompanied by the co …

[HTML][HTML] Plasmodium falciparum resistance to ACTs: Emergence, mechanisms, and outlook

FA Siddiqui, X Liang, L Cui - … Journal for Parasitology: Drugs and Drug …, 2021 - Elsevier
Emergence and spread of resistance in Plasmodium falciparum to the frontline treatment
artemisinin-based combination therapies (ACTs) in the epicenter of multidrug resistance of …

[HTML][HTML] Resistance to artemisinin combination therapies (ACTs): do not forget the partner drug!

C Nsanzabana - Tropical medicine and infectious disease, 2019 - mdpi.com
Artemisinin-based combination therapies (ACTs) have become the mainstay for malaria
treatment in almost all malaria endemic settings. Artemisinin derivatives are highly potent …