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Literature summary for 3.4.23.39 extracted from

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

Crystallization (Commentary)

Crystallization (Comment) Organism
plasmepsin II in complex with isovaleryl pepstatin Plasmodium falciparum

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
Piperidine-4-carboxylic acid {3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
PS-273800
-
Plasmodium falciparum
Ro40-5576
-
Plasmodium falciparum

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
spectrin + H2O Plasmodium falciparum the enzyme catalyzes the degradation of spectrin in the erythrocyte membrane cytoskeletron ?
-
?

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, proplasmepsin II can autoactivate at acidic pH Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
spectrin + H2O
-
Plasmodium falciparum ?
-
?
spectrin + H2O the enzyme catalyzes the degradation of spectrin in the erythrocyte membrane cytoskeletron Plasmodium falciparum ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000004
-
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
0.00005
-
PS-273800
-
Plasmodium falciparum
0.00025
-
Ro40-5576
-
Plasmodium falciparum