Plasmepsin Inhibitory Activity and Structure-Guided Optimization of a Potent Hydroxyethylamine-Based Antimalarial Hit

[Image: see text] Antimalarial hit 1SR (TCMDC-134674) identified in a GlaxoSmithKline cell based screening campaign was evaluated for inhibitory activity against the digestive vacuole plasmepsins (Plm I, II, and IV). It was found to be a potent Plm IV inhibitor with no selectivity over Cathepsin D....

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Bibliografiske detaljer
Main Authors: Jaudzems, Kristaps, Tars, Kaspars, Maurops, Gundars, Ivdra, Natalija, Otikovs, Martins, Leitans, Janis, Kanepe-Lapsa, Iveta, Domraceva, Ilona, Mutule, Ilze, Trapencieris, Peteris, Blackman, Michael J., Jirgensons, Aigars
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2014
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027636/
https://ncbi.nlm.nih.gov/pubmed/24900843
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml4004952
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