A5003418702- Malaria Research and Control
- HIV Research and Treatment
- HIV/AIDS drug development and treatment
- Histone Deacetylase Inhibitors Research
University of Pretoria
2020-2022
Abstract Chemical matter is needed to target the divergent biology associated with different life cycle stages of Plasmodium . Here, we report parallel de novo screening Medicines for Malaria Venture (MMV) Pandemic Response Box against asexual and liver stage parasites, IV/V gametocytes, gametes, oocysts as endectocides. Unique chemotypes were identified both multistage activity or stage-specific activity, including structurally diverse gametocyte-targeted compounds potent...
Abstract The epigenome of the malaria parasite, Plasmodium falciparum , is associated with regulation various essential processes in parasite including control proliferation during asexual development as well sexual differentiation. unusual nature has prompted investigations into potential to target epigenetic modulators novel chemotypes. Here, we explored diversity within a library 95 compounds, active against modifiers cancerous cells, for activity multiple stages P. development. We show...
Malaria elimination requires multipronged approaches, including the application of antimalarial drugs able to block human-to-mosquito transmission malaria parasites. The transmissible gametocytes Plasmodium falciparum seem be highly sensitive towards epidrugs, particularly those targeting demethylation histone post-translational marks. Here, we report exploration compounds from a chemical library generated during hit-to-lead optimization inhibitors human lysine demethylase, KDM4B....