Literature summary for 3.4.23.38 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.

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Cloned(Commentary)

Cloned (Comment)	Organism
expression of proplasmepsin I and V110P-proplasmepsin in Escherichia coli	Plasmodium falciparum
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

Cloned (Comment)

Organism

expression of proplasmepsin I and V110P-proplasmepsin in Escherichia coli

Plasmodium falciparum

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

Protein Variants

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

Inhibitors

Inhibitors	Comment	Organism
isovaleryl-pepstatin	-	Plasmodium falciparum
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide	-	Plasmodium falciparum
Ro40-4388	-	Plasmodium falciparum
Ro40-5576	-	Plasmodium falciparum

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.01	-	Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe	pH 4.4, 37°C	Plasmodium falciparum
0.03	-	Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe	pH 4.4, 37°C	Plasmodium falciparum

Organism

Organism	UniProt	Comment	Textmining
Plasmodium falciparum	-	-	-

Posttranslational Modification

Posttranslational Modification	Comment	Organism
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

Purification (Commentary)

Purification (Comment)	Organism
recombinant V110P-proplasmepsin I	Plasmodium falciparum

Source Tissue

Source Tissue	Comment	Organism	Textmining
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	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.
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	-	?
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe + H2O	-	Plasmodium falciparum	Leu-Glu-Arg-Ile-Phe + Phe(NO2)-Ser-Phe	-	?
Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe + H2O	-	Plasmodium falciparum	Leu-Glu-Arg-Val-Phe + Phe(NO2)-Ser-Phe	-	?

Turnover Number [1/s]

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

pH Optimum

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

pH Range

pH Minimum	pH Maximum	Comment	Organism
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

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism
additional information	-	additional information	Ki-value for Ro17-7109 is above 0.05 mM	Plasmodium falciparum
0.000008	-	Ro40-5576	-	Plasmodium falciparum
0.000009	-	Ro40-4388	-	Plasmodium falciparum
0.0003	-	N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide	-	Plasmodium falciparum