KBE009: An antimalarial bestatin-like inhibitor of the Plasmodium falciparum M1 aminopeptidase discovered in an Ugi multicomponent reaction-derived peptidomimetic library

[Display omitted] Malaria is a global human parasitic disease mainly caused by the protozoon Plasmodium falciparum. Increased parasite resistance to current drugs determines the relevance of finding new treatments against new targets. A novel target is the M1 alanyl-aminopeptidase from P. falciparum...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2017-09, Vol.25 (17), p.4628-4636
Hauptverfasser:	González-Bacerio, Jorge, Maluf, Sarah El Chamy, Méndez, Yanira, Pascual, Isel, Florent, Isabelle, Melo, Pollyana M.S., Budu, Alexandre, Ferreira, Juliana C., Moreno, Ernesto, Carmona, Adriana K., Rivera, Daniel G., Alonso del Rivero, Maday, Gazarini, Marcos L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antimalarials Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Binding Sites Catalytic Domain CD13 Antigens - antagonists & inhibitors CD13 Antigens - genetics CD13 Antigens - metabolism Cell Survival - drug effects Chemical Sciences Combinatorial synthesis Dipeptides - chemical synthesis Dipeptides - chemistry Dipeptides - pharmacology Erythrocytes - cytology Erythrocytes - drug effects Erythrocytes - parasitology Human Umbilical Vein Endothelial Cells Humans Leucine - analogs & derivatives Leucine - chemistry Leucine - pharmacology Metallo-aminopeptidase inhibitors Molecular Docking Simulation Multicomponent reactions Peptidomimetics PfA-M1 Plasmodium falciparum Plasmodium falciparum - drug effects Plasmodium falciparum - enzymology Protozoan Proteins - antagonists & inhibitors Protozoan Proteins - metabolism Recombinant Proteins - biosynthesis Recombinant Proteins - chemistry Recombinant Proteins - isolation & purification Structure-Activity Relationship
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