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Literature summary for 3.4.11.7 extracted from

  • Teuscher, F.; Lowther, J.; Skinner-Adams, T.S.; Spielmann, T.; Dixon, M.W.; Stack, C.M.; Donnelly, S.; Mucha, A.; Kafarski, P.; Vassiliou, S.; Gardiner, D.L.; Dalton, J.P.; Trenholme, K.R.
    The M18 aspartyl aminopeptidase of the human malaria parasite Plasmodium falciparum (2007), J. Biol. Chem., 282, 30817-30826.
    View publication on PubMed

Application

Application Comment Organism
medicine enzyme is a promising target for new anti-malarial drug development Plasmodium falciparum

Cloned(Commentary)

Cloned (Comment) Organism
using codons for optimized gene expression in the yeast Pichia pastoris, for protein expression Sf9 insect cells are infected with PfM18AAP recombinant Baculovirus, furthermore pGEM, pHGFPB and pHcmycB are used Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
(1-aminopropane-1,3-diyl)bis(phosphonic acid)
-
Plasmodium falciparum
(3R)-3-amino-3-phosphonopropanoic acid
-
Plasmodium falciparum
3-amino-3-[hydroxy(phenyl)phosphoryl]propanoic acid
-
Plasmodium falciparum
3-[(1-amino-2-carboxyethyl)(hydroxy)phosphoryl]-2-methylpropanoic acid
-
Plasmodium falciparum
3-[[amino(carboxy)methyl](hydroxy)phosphoryl]-2-methylpropanoic acid
-
Plasmodium falciparum
5-amino-5-phosphonopentanoic acid
-
Plasmodium falciparum
amino(phosphono)acetic acid
-
Plasmodium falciparum
amino[hydroxy(methyl)phosphoryl]acetic acid
-
Plasmodium falciparum
EDTA activity is reduced to 14% after incubating with 10 mM EDTA Plasmodium falciparum
o-phenanthroline activity is reduced to 8.3% after incubating with 20 mM o-phenanthroline Plasmodium falciparum
Zn2+ Zn2+ abolishes enzyme activity at a concentration of 1 mM Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.1351
-
Glu-7-amido-4-methylcoumarin in the absence of cobalt Plasmodium falciparum
0.1363
-
Glu-7-amido-4-methylcoumarin in the presence of 1 mM cobalt Plasmodium falciparum
0.3273
-
Asp-7-amido-4-methylcoumarin in the presence of 1 mM cobalt Plasmodium falciparum
0.3848
-
Asp-7-amido-4-methylcoumarin in the absence of cobalt Plasmodium falciparum

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Plasmodium falciparum 5829
-
vacuole
-
Plasmodium falciparum 5773
-

Metals/Ions

Metals/Ions Comment Organism Structure
Co2+
-
Plasmodium falciparum

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
65000
-
determined by reducing SDS-PAGE Plasmodium falciparum
560000
-
octamer, determined by gel filtration HPLC on a Superdex-200 column Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q8I2J3
-
-

Purification (Commentary)

Purification (Comment) Organism
by affinity chromatography on a Ni-NTA column Plasmodium falciparum

Source Tissue

Source Tissue Comment Organism Textmining
ring stage
-
Plasmodium falciparum
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
607
-
Glu-7-amido-4-methylcoumarin Plasmodium falciparum
662.5
-
Asp-7-amido-4-methylcoumarin Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Asp-7-amido-4-methylcoumarin + H2O assay for measuring aspartyl aminopeptidase activity Plasmodium falciparum Asp + 7-amino-4-methylcoumarin
-
?
Glu-7-amido-4-methylcoumarin + H2O assay for measuring aspartyl aminopeptidase activity Plasmodium falciparum Glu + 7-amino-4-methylcoumarin
-
?
Leu-7-amido-4-methylcoumarin + H2O assay for measuring aspartyl aminopeptidase activity Plasmodium falciparum Leu + 7-amino-4-methylcoumarin
-
?

Subunits

Subunits Comment Organism
octamer
-
Plasmodium falciparum

Synonyms

Synonyms Comment Organism
Aminopeptidase
-
Plasmodium falciparum
aspartyl aminopeptidase
-
Plasmodium falciparum
M18 aspartyl aminopeptidase
-
Plasmodium falciparum

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
activity assay Plasmodium falciparum

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.011
-
Glu-7-amido-4-methylcoumarin in the absence of cobalt Plasmodium falciparum
0.05
-
Asp-7-amido-4-methylcoumarin in the absence of cobalt Plasmodium falciparum
0.33
-
Glu-7-amido-4-methylcoumarin in the presence of 1 mM cobalt Plasmodium falciparum
0.354
-
Asp-7-amido-4-methylcoumarin in the presence of 1 mM cobalt Plasmodium falciparum

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
activity assay Plasmodium falciparum

pH Range

pH Minimum pH Maximum Comment Organism
6 9
-
Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00034
-
(3R)-3-amino-3-phosphonopropanoic acid
-
Plasmodium falciparum
0.0044
-
(1-aminopropane-1,3-diyl)bis(phosphonic acid)
-
Plasmodium falciparum
0.0271
-
amino(phosphono)acetic acid
-
Plasmodium falciparum
0.0427
-
3-[(1-amino-2-carboxyethyl)(hydroxy)phosphoryl]-2-methylpropanoic acid
-
Plasmodium falciparum
0.105
-
5-amino-5-phosphonopentanoic acid
-
Plasmodium falciparum
0.1831
-
3-[[amino(carboxy)methyl](hydroxy)phosphoryl]-2-methylpropanoic acid
-
Plasmodium falciparum
0.395
-
amino[hydroxy(methyl)phosphoryl]acetic acid
-
Plasmodium falciparum
2
-
3-amino-3-[hydroxy(phenyl)phosphoryl]propanoic acid
-
Plasmodium falciparum