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 …

Beyond PI3Ks: targeting phosphoinositide kinases in disease

JE Burke, J Triscott, BM Emerling… - Nature Reviews Drug …, 2023 - nature.com
Lipid phosphoinositides are master regulators of almost all aspects of a cell's life and death
and are generated by the tightly regulated activity of phosphoinositide kinases. Although …

Antimalarial drug resistance and implications for the WHO global technical strategy

MM Ippolito, KA Moser, JBB Kabuya… - Current epidemiology …, 2021 - Springer
Abstract Purpose of Review Five years have passed since the World Health Organization
released its Global Technical Strategy for Malaria (GTS). In that time, progress against …

The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages

LB Arendse, JM Murithi, T Qahash… - Science translational …, 2022 - science.org
Compounds acting on multiple targets are critical to combating antimalarial drug resistance.
Here, we report that the human “mammalian target of rapamycin”(mTOR) inhibitor …

2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy

GA Dziwornu, D Seanego, S Fienberg… - Journal of Medicinal …, 2024 - ACS Publications
Structure–activity relationship studies of 2, 8-disubstituted-1, 5-naphthyridines, previously
reported as potent inhibitors of Plasmodium falciparum (Pf) phosphatidylinositol-4-kinase β …

The development process for discovery and clinical advancement of modern antimalarials

TD Ashton, SM Devine, JJ Mohrle, B Laleu… - Journal of Medicinal …, 2019 - ACS Publications
Malaria is a devastating disease caused by Plasmodium parasites, resulting in
approximately 435000 deaths in 2018. The impact of malaria is compounded by the …

The Great Escape: how phosphatidylinositol 4-kinases and PI4P promote vesicle exit from the Golgi (and drive cancer)

MG Waugh - Biochemical journal, 2019 - portlandpress.com
Abstract Phosphatidylinositol 4-phosphate (PI4P) is a membrane glycerophospholipid and a
major regulator of the characteristic appearance of the Golgi complex as well as its vesicular …

Targeting malaria parasite invasion of red blood cells as an antimalarial strategy

AL Burns, MG Dans, JM Balbin… - FEMS microbiology …, 2019 - academic.oup.com
Plasmodium spp. parasites that cause malaria disease remain a significant global-health
burden. With the spread of parasites resistant to artemisinin combination therapies in …

Advances in malaria pharmacology and the online guide to MALARIA PHARMACOLOGY: IUPHAR review 38

JF Armstrong, B Campo, SPH Alexander… - British Journal of …, 2023 - Wiley Online Library
Antimalarial drug discovery has until recently been driven by high‐throughput phenotypic
cellular screening, allowing millions of compounds to be assayed and delivering clinical …

Parasite and host kinases as targets for antimalarials

HW Ong, J Adderley, AB Tobin… - Expert Opinion on …, 2023 - Taylor & Francis
ABSTRACT Introduction The deployment of Artemisinin-based combination therapies and
transmission control measures led to a decrease in the global malaria burden over the …