Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti‐malaria Activity in Humanized Mice

Plasmodium falciparum proteasome (Pf20S) inhibitors are active against Plasmodium at multiple stages—erythrocytic, gametocyte, liver, and gamete activation stages—indicating that selective Pf20S inhibitors possess the potential to be therapeutic, prophylactic, and transmission‐blocking antimalarials...

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Veröffentlicht in:	Angewandte Chemie International Edition 2021-04, Vol.60 (17), p.9279-9283
Hauptverfasser:	Zhan, Wenhu, Zhang, Hao, Ginn, John, Leung, Annie, Liu, Yi J., Michino, Mayako, Toita, Akinori, Okamoto, Rei, Wong, Tzu‐Tshin, Imaeda, Toshihiro, Hara, Ryoma, Yukawa, Takafumi, Chelebieva, Sevil, Tumwebaze, Patrick K., Lafuente‐Monasterio, Maria Jose, Martinez‐Martinez, Maria Santos, Vendome, Jeremie, Beuming, Thijs, Sato, Kenjiro, Aso, Kazuyoshi, Rosenthal, Philip J., Cooper, Roland A., Meinke, Peter T., Nathan, Carl F., Kirkman, Laura A., Lin, Gang
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Artemisinin Drug Development Erythrocytes Gametocytes Inhibitors Malaria Malaria, Falciparum - drug therapy Malaria, Falciparum - metabolism Mice Models, Molecular Molecular Conformation Parasitemia Parasitic Sensitivity Tests Peptide inhibitors Pharmacokinetics Plasmodium falciparum Plasmodium falciparum - drug effects Plasmodium falciparum - enzymology proteasome Proteasome Endopeptidase Complex - metabolism Proteasome inhibitors Proteasome Inhibitors - chemical synthesis Proteasome Inhibitors - chemistry Proteasome Inhibitors - pharmacology Selectivity therapeutics Vector-borne diseases
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