Antimalarial drug discovery: Progress and approaches
Recent antimalarial drug discovery has been a race to produce new medicines that
overcome emerging drug resistance, whilst considering safety and improving dosing …
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 …
and are generated by the tightly regulated activity of phosphoinositide kinases. Although …
Antimalarial drug resistance and implications for the WHO global technical strategy
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 …
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 …
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 …
reported as potent inhibitors of Plasmodium falciparum (Pf) phosphatidylinositol-4-kinase β …
The development process for discovery and clinical advancement of modern antimalarials
Malaria is a devastating disease caused by Plasmodium parasites, resulting in
approximately 435000 deaths in 2018. The impact of malaria is compounded by the …
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 …
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 …
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 …
cellular screening, allowing millions of compounds to be assayed and delivering clinical …
Parasite and host kinases as targets for antimalarials
ABSTRACT Introduction The deployment of Artemisinin-based combination therapies and
transmission control measures led to a decrease in the global malaria burden over the …
transmission control measures led to a decrease in the global malaria burden over the …