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Literature summary for 3.4.23.38 extracted from

  • Berry, C.
    Plasmepsins as antimalarial targets (2000), Curr. Opin. Drug Discov. Devel., 3, 624-629.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
17-benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16-tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
Plasmodium falciparum
additional information none of the inhibitors analyzed to date have sufficient selectivity for plasmepsin I and II, compared to their human counterparts Plasmodium falciparum
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification the proenzyme has an unusually long propart of 125 amino acid residues that mediates type II membrane anchoring of the proenzyme, activation occurs by removal of the propart Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000001
-
17-Benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
Plasmodium falciparum
0.000006
-
Ro40-5576
-
Plasmodium falciparum