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Literature summary for 3.4.23.B19 extracted from
- Structural basis for plasmepsin V inhibition that blocks export of malaria proteins to human erythrocytes (2015), Nat. Struct. Mol. Biol., 22, 590-596 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in High Five insect cells | Plasmodium vivax |
| expressed in Sf21 insect cells | Plasmodium falciparum |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| WEHI-842 | potent inhibitor | Plasmodium falciparum |  |
| WEHI-842 | potent inhibitor | Plasmodium vivax | |
| WEHI-916 | - |
Plasmodium falciparum | |
| WEHI-916 | - |
Plasmodium vivax | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00693 | - |
Dabcyl-RNKRTLAQKQ-E-Edans | at pH 6.4 and 37°C | Plasmodium vivax | |
| 0.02443 | - |
Dabcyl-RNKRTLAQKQ-E-Edans | at pH 6.4 and 37°C | Plasmodium falciparum | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Plasmodium falciparum | Q8I6Z5 | isolate 3D7 | - |
| Plasmodium vivax | Q6PRR9 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| Superdex 75 gel filtration | Plasmodium falciparum |
| Superdex 75 gel filtration | Plasmodium vivax |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Dabcyl-RNKKTLAQKQ-E-Edans + H2O | - |
Plasmodium falciparum | ? | - |
? | |
| Dabcyl-RNKKTLAQKQ-E-Edans + H2O | - |
Plasmodium vivax | ? | - |
? | |
| Dabcyl-RNKRTIAQKQ-E-Edans + H2O | - |
Plasmodium falciparum | ? | - |
? | |
| Dabcyl-RNKRTIAQKQ-E-Edans + H2O | - |
Plasmodium vivax | ? | - |
? | |
| Dabcyl-RNKRTLAQKQ-E-Edans + H2O | - |
Plasmodium falciparum | ? | - |
? | |
| Dabcyl-RNKRTLAQKQ-E-Edans + H2O | - |
Plasmodium vivax | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PMV | - |
Plasmodium falciparum |
| PMV | - |
Plasmodium vivax |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 1.86 | - |
Dabcyl-RNKRTLAQKQ-E-Edans | at pH 6.4 and 37°C | Plasmodium falciparum | |
| 3.64 | - |
Dabcyl-RNKRTLAQKQ-E-Edans | at pH 6.4 and 37°C | Plasmodium vivax | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000002 | - |
at pH 6.4 and 37°C | Plasmodium falciparum | WEHI-842 | |
| 0.0000004 | - |
at pH 6.4 and 37°C | Plasmodium vivax | WEHI-842 | |
| 0.0000021 | - |
at pH 6.4 and 37°C | Plasmodium vivax | WEHI-916 | |
| 0.0000035 | - |
at pH 6.4 and 37°C | Plasmodium falciparum | WEHI-916 | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | plasmepsin V inhibition blocks export of malaria proteins to human erythrocytes and inhibits parasite growth | Plasmodium falciparum |
| malfunction | plasmepsin V inhibition blocks export of malaria proteins to human erythrocytes and inhibits parasite growth | Plasmodium vivax |
kcat/KM [mM/s]
| kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 80 | - |
Dabcyl-RNKRTLAQKQ-E-Edans | at pH 6.4 and 37°C | Plasmodium falciparum | |
| 530 | - |
Dabcyl-RNKRTLAQKQ-E-Edans | at pH 6.4 and 37°C | Plasmodium vivax | |
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