Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase

…, S Ferrer, LM Sanz, FJ Gamo, J Reader… - Science translational …, 2017 - science.org
As part of the global effort toward malaria eradication, phenotypic whole-cell screening
revealed the 2-aminopyridine class of small molecules as a good starting point to develop new …

[HTML][HTML] Nowhere to hide: interrogating different metabolic parameters of Plasmodium falciparum gametocytes in a transmission blocking drug discovery pipeline …

J Reader, M Botha, A Theron, SB Lauterbach… - Malaria journal, 2015 - Springer
Background The discovery of malaria transmission-blocking compounds is seen as key to
malaria elimination strategies and gametocyte-screening platforms are critical filters to identify …

[HTML][HTML] A dynamic and combinatorial histone code drives malaria parasite asexual and sexual development

…, M Coradin, MR Mendoza, J Reader… - Molecular & Cellular …, 2022 - ASBMB
Histone posttranslational modifications (PTMs) frequently co-occur on the same chromatin
domains or even in the same molecule. It is now established that these "histone codes" are …

Benzimidazole Derivatives Are Potent against Multiple Life Cycle Stages of Plasmodium falciparum Malaria Parasites

…, GA Dziwornu, D Coertzen, J Reader… - ACS Infectious …, 2021 - ACS Publications
The continued emergence of resistance to front-line antimalarial treatments is of great concern.
Therefore, new compounds that potentially have a novel target in various developmental …

[HTML][HTML] Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites

…, D Opperman, M van der Watt, J Reader… - Scientific reports, 2020 - nature.com
The epigenome of the malaria parasite, Plasmodium falciparum, is associated with regulation
of various essential processes in the parasite including control of proliferation during …

[HTML][HTML] Adapt or die: targeting unique transmission-stage biology for malaria elimination

ME van der Watt, J Reader… - Frontiers in Cellular and …, 2022 - frontiersin.org
Plasmodium parasites have a complex life cycle that includes development in the human host
as well as the Anopheles vector. Successful transmission of the parasite between its host …

[HTML][HTML] Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box

J Reader, ME van der Watt, D Taylor… - Nature …, 2021 - nature.com
Chemical matter is needed to target the divergent biology associated with the different life
cycle stages of Plasmodium. Here, we report the parallel de novo screening of the Medicines …

[HTML][HTML] Hierarchical transcriptional control regulates Plasmodium falciparum sexual differentiation

…, R Van Wyk, HJ Painter, L Orchard, J Reader… - BMC genomics, 2019 - Springer
Background Malaria pathogenesis relies on sexual gametocyte forms of the malaria parasite
to be transmitted between the infected human and the mosquito host but the molecular …

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

…, D Coertzen, M van der Watt, J Reader… - 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 …

UCT943, a next-generation Plasmodium falciparum PI4K inhibitor preclinical candidate for the treatment of malaria

…, TL Coetzer, ME Van der Watt, J Reader… - Antimicrobial agents …, 2018 - Am Soc Microbiol
The 2-aminopyridine MMV048 was the first drug candidate inhibiting Plasmodium
phosphatidylinositol 4-kinase (PI4K), a novel drug target for malaria, to enter clinical development. In …