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 …

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 …

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 …

Drugs in development for malaria

EA Ashley, AP Phyo - Drugs, 2018 - Springer
The last two decades have seen a surge in antimalarial drug development with product
development partnerships taking a leading role. Resistance of Plasmodium falciparum to the …

Structural basis for regulation of phosphoinositide kinases and their involvement in human disease

JE Burke - Molecular cell, 2018 - cell.com
Lipid phosphoinositides play fundamental roles in virtually all pathways that control a cell's
decision to grow, move, divide, and die. Because of this, kinases that phosphorylate …

Challenges and recent progress in drug discovery for tropical diseases

M De Rycker, B Baragaña, SL Duce, IH Gilbert - Nature, 2018 - nature.com
Infectious tropical diseases have a huge effect in terms of mortality and morbidity, and
impose a heavy economic burden on affected countries. These diseases predominantly …

Novel roles of phosphoinositides in signaling, lipid transport, and disease

GRV Hammond, JE Burke - Current Opinion in Cell Biology, 2020 - Elsevier
Phosphoinositides (PPIns) are lipid signaling molecules that act as master regulators of
cellular signaling. Recent studies have revealed novel roles of PPIns in myriad cellular …

Current development of 1, 2, 3-triazole derived potential antimalarial scaffolds: Structure activity relationship (SAR) and bioactive compounds

SMA Rahman, JS Bhatti, S Thareja, V Monga - European Journal of …, 2023 - Elsevier
Malaria is among one of the most devastating and deadliest parasitic disease in the world
claiming millions of lives every year around the globe. It is a mosquito-borne infectious …

[HTML][HTML] First fully-automated AI/ML virtual screening cascade implemented at a drug discovery centre in Africa

G Turon, J Hlozek, JG Woodland, A Kumar… - Nature …, 2023 - nature.com
Streamlined data-driven drug discovery remains challenging, especially in resource-limited
settings. We present ZairaChem, an artificial intelligence (AI)-and machine learning (ML) …

Assessing risks of Plasmodium falciparum resistance to select next-generation antimalarials

M Duffey, B Blasco, JN Burrows, TNC Wells… - Trends in …, 2021 - cell.com
Strategies to counteract or prevent emerging drug resistance are crucial for the design of
next-generation antimalarials. In the past, resistant parasites were generally identified …