Antiplasmodial Mode of Action of Pantothenamides: Pantothenate Kinase Serves as a Metabolic Activator Not as a Target

N-Substituted pantothenamides (PanAms) are pantothenate analogues with up to nanomolar potency against blood-stage Plasmodium falciparum (the most virulent species responsible for malaria). Although these compounds are known to target coenzyme A (CoA) biosynthesis and/or utilization, their exact mod...

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Veröffentlicht in:	ACS infectious diseases 2017-07, Vol.3 (7), p.527-541
Hauptverfasser:	de Villiers, Marianne, Spry, Christina, Macuamule, Cristiano J, Barnard, Leanne, Wells, Gordon, Saliba, Kevin J, Strauss, Erick
Format:	Artikel
Sprache:	eng
Schlagworte:	Antimalarials - chemical synthesis Antimalarials - metabolism Antimalarials - pharmacology Antimetabolites - metabolism Antimetabolites - pharmacology beta-Alanine - analogs & derivatives beta-Alanine - metabolism beta-Alanine - pharmacology Biotransformation Carbon Radioisotopes Coenzyme A - antagonists & inhibitors Coenzyme A - biosynthesis Erythrocytes - drug effects Erythrocytes - parasitology Humans Kinetics Models, Molecular Pantothenic Acid - analogs & derivatives Pantothenic Acid - metabolism Pantothenic Acid - pharmacology Parasitic Sensitivity Tests Phosphorylation Phosphotransferases (Alcohol Group Acceptor) - metabolism Plasmodium falciparum - drug effects Plasmodium falciparum - growth & development Plasmodium falciparum - metabolism Protein Binding Protozoan Proteins - metabolism Structure-Activity Relationship
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