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Literature summary for 3.4.23.38 extracted from

  • Liu, P.; Marzahn, M.; Robbins, A.; Gutierrez-de-Teran, H.; Rodriguez, D.; McClung, S.; Stevens, S.; Yowell, C.; Dame, J.; McKenna, R.; Dunn, B.
    Recombinant plasmepsin 1 from the human malaria parasite Plasmodium falciparum: Enzymatic characterization, active site inhibitor design, and structural analysis (2009), Biochemistry, 48, 4086-99.
    View publication on PubMedView publication on EuropePMC
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Cloned(Commentary)

Cloned (Comment) Organism
expression of truncated proPfPM1 K110pN mutant in Escherichia coli Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
KPFEL-PSI(CH2-NH)-AWT combinatorial chemistry derived peptide inhibitor Plasmodium falciparum
KPFSL-PSI(CH2-NH)-LQF combinatorial chemistry derived peptide inhibitor, 5fold selectivity over human cathepsin D Plasmodium falciparum
KPLEF-PSI(CH2-NH)-FRV combinatorial chemistry derived peptide inhibitor Plasmodium falciparum
KPLEF-PSI(CH2-NH)-YRV combinatorial chemistry derived peptide inhibitor Plasmodium falciparum
KPnorLSnorL-PSI(CH2-NH)-LQI combinatorial chemistry derived peptide inhibitor Plasmodium falciparum
KPVEF-PSI(CH2-NH)-RQT combinatorial chemistry derived peptide inhibitor Plasmodium falciparum
pepstatin A
-
 Plasmodium falciparum
Ro40-4388
-
 Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0086
-
 Leu-Glu-Arg-Ile-Phe-(p-nitro)Phe-Ser-Phe pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
0.009
-
 Lys-Glu-Leu-Val-Phe-(p-nitro)Phe-Ala-Leu-Lys pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
0.0132
-
 Lys-Pro-Ile-Leu-Phe-(p-nitro)Phe-Arg-Leu pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum P39898
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification automaturation of proPfPM1 K110pN mutant at pH 4.0-4.5, with reduction of molecular weight by 5 kDa Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Leu-Glu-Arg-Ile-Phe-(p-nitro)Phe-Ser-Phe + H2O
-
 Plasmodium falciparum Leu-Glu-Arg-Ile-Phe + (p-nitro)Phe-Ser-Phe
-
 ?
Lys-Glu-Leu-Val-Phe-(p-nitro)Phe-Ala-Leu-Lys + H2O
-
 Plasmodium falciparum Lys-Glu-Leu-Val-Phe + (p-nitro)Phe-Ala-Leu-Lys
-
 ?
Lys-Pro-Ile-Leu-Phe-(p-nitro)Phe-Arg-Leu + H2O
-
 Plasmodium falciparum Lys-Pro-Ile-Leu-Phe + (p-nitro)Phe-Arg-Leu
-
 ?
additional information S1' subsite prefers hydrophobic residues and the S2' subsite shifts its preferences more to polar residues. Serine is a preferred P1' substitution Plasmodium falciparum ?
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.1
-
 Lys-Pro-Ile-Leu-Phe-(p-nitro)Phe-Arg-Leu pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
2.6
-
 Leu-Glu-Arg-Ile-Phe-(p-nitro)Phe-Ser-Phe pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
2.9
-
 Lys-Glu-Leu-Val-Phe-(p-nitro)Phe-Ala-Leu-Lys pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
4.5
-
 recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000014
-
 pepstatin A pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
0.0000014
-
 Ro40-4388 pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
0.000043
-
 KPFSL-PSI(CH2-NH)-LQF pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
0.000073
-
 KPnorLSnorL-PSI(CH2-NH)-LQI pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
0.0055
-
 KPLEF-PSI(CH2-NH)-FRV pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
0.031
-
 KPVEF-PSI(CH2-NH)-RQT pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
0.038
-
 KPLEF-PSI(CH2-NH)-YRV pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
0.042
-
 KPFEL-PSI(CH2-NH)-AWT pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum