Malaria parasite plasmepsins: More than just plain old degradative pepsins

AS Nasamu, AJ Polino, ES Istvan… - Journal of Biological …, 2020 - ASBMB
Plasmepsins are a group of diverse aspartic proteases in the malaria parasite Plasmodium.
Their functions are strikingly multifaceted, ranging from hemoglobin degradation to secretory …

Proteases as antimalarial targets: strategies for genetic, chemical, and therapeutic validation

E Deu - The FEBS journal, 2017 - Wiley Online Library
Malaria is a devastating parasitic disease affecting half of the world's population. The rapid
emergence of resistance against new antimalarial drugs, including artemisinin‐based …

Plasmepsin inhibitors in antimalarial drug discovery: medicinal chemistry and target validation (2000 to present)

PM Cheuka, G Dziwornu, J Okombo… - Journal of medicinal …, 2020 - ACS Publications
Plasmepsins represent novel antimalarial drug targets. However, plasmepsin-based
antimalarial drug discovery efforts in the past 2 decades have generally suffered some …

Transition State Mimetics of the Plasmodium Export Element Are Potent Inhibitors of Plasmepsin V from P. falciparum and P. vivax

BE Sleebs, M Gazdik, MT O'Neill… - Journal of medicinal …, 2014 - ACS Publications
Following erythrocyte invasion, malaria parasites export a catalogue of remodeling proteins
into the infected cell that enable parasite development in the human host. Export is …

Inhibitors of Plasmepsin X Plasmodium falciparum: Structure-based pharmacophore generation and molecular dynamics simulation

SK Panda, S Saxena, PSS Gupta, MK Rana - Journal of Molecular Liquids, 2021 - Elsevier
Malaria is a life-threatening disease caused by Plasmodium parasites, which are transmitted
to humans through infected female Anopheles mosquitoes. Over the past few decades …

Plasmodium falciparum ookinete expression of plasmepsin VII and plasmepsin X

F Li, V Bounkeua, K Pettersen, JM Vinetz - Malaria Journal, 2016 - Springer
Background Plasmodium invasion of the mosquito midgut is a population bottleneck in the
parasite lifecycle. Interference with molecular mechanisms by which the ookinete invades …

Exploiting structural dynamics to design open-flap inhibitors of malarial aspartic proteases

R Bobrovs, K Jaudzems… - Journal of Medicinal …, 2019 - ACS Publications
Malaria is a life-threatening infectious disease caused by Plasmodium parasites.
Plasmepsins (proteolytic enzymes of the parasite) have been considered as promising …

Parasite cathepsin D-like peptidases and their relevance as therapeutic targets

D Sojka, D Hartmann, P Bartošová-Sojková… - Trends in …, 2016 - cell.com
Inhibition of aspartic cathepsin D-like peptidases (APDs) has been often discussed as an
antiparasite intervention strategy. APDs have been considered as virulence factors of …

Plasmepsin-like Aspartyl Proteases in Babesia

P Šnebergerová, P Bartošová-Sojková, M Jalovecká… - Pathogens, 2021 - mdpi.com
Apicomplexan genomes encode multiple pepsin-family aspartyl proteases (APs) that
phylogenetically cluster to six independent clades (A to F). Such diversification has been …

Enhanced antimalarial activity of plasmepsin V inhibitors by modification of the P2 position of PEXEL peptidomimetics

W Nguyen, AN Hodder, RB de Lezongard… - European Journal of …, 2018 - Elsevier
Plasmepsin V is an aspartyl protease that plays a critical role in the export of proteins
bearing the Plasmodium export element (PEXEL) motif (RxLxQ/E/D) to the infected host …