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Literature summary extracted from

  • Moon, R.P.; Tyas, L.; Certa, U.; Rupp, K.; Bur, D.; Jacquet, C.; Matile, H.; Loetscher, H.; Grueninger-Leitch, F.; et al.
    Expression and characterization of plasmepsin I from Plasmodium falciparum (1997), Eur. J. Biochem., 244, 552-560.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.23.38 expression of proplasmepsin I and V110P-proplasmepsin in Escherichia coli Plasmodium falciparum
3.4.23.38 initial attempts to express full-length proplasmepsin I gene in Escherichia coli results in very low expression levels, possibly due to the toxic effects of the hydrophobic segment, and no activation to mature plasmepsin I is ever observed. Recombinant proplasmepsin I is expressed from pETPMI, a construct that is prepared from pET3a and contains the last 48 residues of the propart followed by the 328 residues of mature plasmepsin I. It is necessary to introduce a processing site, V110P, into the zymogen that renders the precursor capable of undergoing autoactivation Plasmodium falciparum
3.4.23.39
-
 Plasmodium falciparum

Protein Variants

EC Number Protein Variants Comment Organism
3.4.23.38 V110P mutation in proplasmepsin I is responsible for generating a form of proplasmepsin I that is capable of undergoing autoactivation Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.23.38 isovaleryl-pepstatin
-
 Plasmodium falciparum
3.4.23.38 N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
 Plasmodium falciparum
3.4.23.38 Ro40-4388
-
 Plasmodium falciparum
3.4.23.38 Ro40-5576
-
 Plasmodium falciparum
3.4.23.39 N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
 Plasmodium falciparum
3.4.23.39 Ro17-7109
-
 Plasmodium falciparum
3.4.23.39 Ro40-4388
-
 Plasmodium falciparum
3.4.23.39 Ro40-5576
-
 Plasmodium falciparum

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.23.38 0.01
-
 Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe pH 4.4, 37°C Plasmodium falciparum
3.4.23.38 0.03
-
 Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe pH 4.4, 37°C Plasmodium falciparum
3.4.23.39 0.02
-
 Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys pH 4.4, 37°C Plasmodium falciparum
3.4.23.39 0.025
-
 Lys-Glu-Phe-Ile-Phe-Phe(NO2)-Ala-Leu-Lys pH 4.4, 37°C Plasmodium falciparum

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 plasmepsin I is produced as a precursor. The propart region, about 120 residues, is more than twice as long as those of archetypal zymogens Plasmodium falciparum
3.4.23.39 proteolytic modification plasmepsin II is produced as a precursor. The propart region, about 120 residues, is more than twice as long as those of archetypal zymogens Plasmodium falciparum

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.23.38 recombinant V110P-proplasmepsin I Plasmodium falciparum
3.4.23.39 proplasmepsin Plasmodium falciparum

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.23.38 additional information proplasmepsin I is expressed in the ring stages whereas the proplasmepsin II gene is not transcribed until the later trophozoite stage of parasite growth Plasmodium falciparum
-
3.4.23.39 trophozoite the proplasmepsin II gene is not transcribed until the later trophozoite stage of parasite growth Plasmodium falciparum
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.23.38 Ala-Leu-Glu-Arg-Thr-Phe-Leu-Ser-Phe-Pro-Thr + H2O
-
 Plasmodium falciparum Ala-Leu-Glu-Arg-Thr-Phe + Leu-Ser-Phe-Pro-Thr
-
 ?
3.4.23.38 Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe + H2O
-
 Plasmodium falciparum Leu-Glu-Arg-Ile-Phe + Phe(NO2)-Ser-Phe
-
 ?
3.4.23.38 Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe + H2O
-
 Plasmodium falciparum Leu-Glu-Arg-Val-Phe + Phe(NO2)-Ser-Phe
-
 ?
3.4.23.39 Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe + H2O
-
 Plasmodium falciparum Leu-Glu-Arg-Ile-Phe + Phe(NO2)-Ser-Phe
-
 ?
3.4.23.39 Lys-Glu-Phe-Ile-Phe-Phe(NO2)-Ala-Leu-Lys + H2O
-
 Plasmodium falciparum Lys-Glu-Phe-Ile-Phe + Phe(NO2)-Ala-Leu-Lys
-
 ?
3.4.23.39 Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys + H2O
-
 Plasmodium falciparum Lys-Glu-Phe-Val-Phe + Phe(NO2)-Ala-Leu-Lys
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.23.38 1.3
-
 Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe pH 4.4, 37°C Plasmodium falciparum
3.4.23.38 1.6
-
 Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe pH 4.4, 37°C Plasmodium falciparum
3.4.23.39 9.05
-
 Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys pH 4.4, 37°C Plasmodium falciparum
3.4.23.39 15.2
-
 Lys-Glu-Phe-Ile-Phe-Phe(NO2)-Ala-Leu-Lys pH 4.4, 37°C Plasmodium falciparum

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.23.38 4
-
 hydrolysis of Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe Plasmodium falciparum

pH Range

EC Number pH Minimum pH Maximum Comment Organism
3.4.23.38 3.5 6 pH 3.5: about 75% of maximal activity, pH 6.0: about 40% of maximal activity, hydrolysis of Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe Plasmodium falciparum
3.4.23.39 3.5 6 pH 3.5: about 65% of maximal activity, pH 6.0: about 30% of maximal activity, hydrolysis of Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.23.38 additional information
-
 additional information Ki-value for Ro17-7109 is above 0.05 mM Plasmodium falciparum
3.4.23.38 0.000008
-
 Ro40-5576
-
 Plasmodium falciparum
3.4.23.38 0.000009
-
 Ro40-4388
-
 Plasmodium falciparum
3.4.23.38 0.0003
-
 N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
 Plasmodium falciparum
3.4.23.39 additional information
-
 additional information the Ki-value for Ro17-7109 is above 0.015 mM Plasmodium falciparum
3.4.23.39 0.00025
-
 Ro40-5576 pH 4.4, 37°C Plasmodium falciparum
3.4.23.39 0.0007
-
 Ro40-4388 pH 4.4, 37°C Plasmodium falciparum
3.4.23.39 0.004
-
 N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide pH 4.4, 37°C Plasmodium falciparum