253 posters, 14 videos, 27 audios, 14 topics, 392 authors, 132 institutions
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4th Commonwealth Chemistry Posters
October 4 - 5, 2023 | Online, United Kingdom
P152
Anticancer Inhibitors of Plasmodium PI4K as Potential Antimalarial Agents
Poster Presenter
Authors
Natalia Shakela, Lauren Arendse, John Woodland, Kathryn Wicht, Kelly Chibale
Affiliations
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa, Holistic Drug Discovery and Development (H3D) Centre, University of Cape Town; South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry and Holistic Drug Discovery and Development (H3D) Centre, University of Cape Town; South African Medical Research Council Drug Discovery and Development Research Unit
Part of Topic
Good health and well-being
Audio
ANTICANCER INHIBITORS OF PLASMODIUM PI4K AS POTENTIAL ANTIMALARIAL AGENTS
95% of all cases of malaria infection that were reported in 2021 occurred in Africa. Drug repositioning refers to using a compound from one disease indication as a template for chemical optimisation against a new indication. In the current work the anticancer agent VE-821 is investigated for repositioning against malaria.VE-821 is a potent anticancer ataxia telangiectasia and Rad3-related kinase inhibitor (ATR). Kinobead screening identified VE-821 as a putative phosphatidylinositol 4-kinase (PI4K) inhibitor. The antimalarial agent MMV390048, which reached Phase IIa clinical trials, is an inhibitor of Plasmodium falciparum (Pf) PI4Kβ. The current objectives are to:
1. Design and synthesise analogues of VE-821.
2. Evaluate analogues in vitro against Pf whole-cell parasites and enzyme Plasmodium vivax (Pv) PI4K.
3. Employ computational tools to deduce structure activity relationships (SAR) and investigate structure property relationships (SPR).