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Literature summary extracted from
- Plasmepsins as antimalarial targets (2000), Curr. Opin. Drug Discov. Devel., 3, 624-629.
Crystallization (Commentary)
| EC Number | Crystallization (Comment) | Organism |
|---|---|---|
| 3.4.23.39 | plasmepsin II in complex with isovaleryl pepstatin | Plasmodium falciparum |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.23.38 | 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 |  |
| 3.4.23.38 | additional information | none of the inhibitors analyzed to date have sufficient selectivity for plasmepsin I and II, compared to their human counterparts | Plasmodium falciparum | |
| 3.4.23.38 | piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide | - |
Plasmodium falciparum | |
| 3.4.23.39 | 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 | |
| 3.4.23.39 | additional information | none of the inhibitors analyzed to date have sufficient selectivity for plasmepsin I and II, compared to their human counterparts | Plasmodium falciparum | |
| 3.4.23.39 | piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide | - |
Plasmodium falciparum | |
| 3.4.23.39 | Piperidine-4-carboxylic acid {3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-[2-(4-methoxy-phenyl)-ethyl]-amide | - |
Plasmodium falciparum | |
| 3.4.23.39 | PS-273800 | - |
Plasmodium falciparum | |
| 3.4.23.39 | Ro40-5576 | - |
Plasmodium falciparum | |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.23.39 | spectrin + H2O | Plasmodium falciparum | the enzyme catalyzes the degradation of spectrin in the erythrocyte membrane cytoskeletron | ? | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.4.23.38 | Plasmodium falciparum | - |
- |
- |
| 3.4.23.39 | Plasmodium falciparum | - |
- |
- |
Posttranslational Modification
| EC Number | Posttranslational Modification | Comment | Organism |
|---|---|---|---|
| 3.4.23.38 | 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 |
| 3.4.23.39 | 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)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.23.39 | spectrin + H2O | - |
Plasmodium falciparum | ? | - |
? | |
| 3.4.23.39 | spectrin + H2O | the enzyme catalyzes the degradation of spectrin in the erythrocyte membrane cytoskeletron | Plasmodium falciparum | ? | - |
? | |
Ki Value [mM]
| EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.4.23.38 | 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 | |
| 3.4.23.38 | 0.000006 | - |
Ro40-5576 | - |
Plasmodium falciparum | |
| 3.4.23.39 | 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 | |
| 3.4.23.39 | 0.00005 | - |
PS-273800 | - |
Plasmodium falciparum | |
| 3.4.23.39 | 0.00025 | - |
Ro40-5576 | - |
Plasmodium falciparum | |
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