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Literature summary 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

Cloned(Commentary)

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

Inhibitors

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

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.23.38 0.0086
-
 Leu-Glu-Arg-Ile-Phe-(p-nitro)Phe-Ser-Phe pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
3.4.23.38 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
3.4.23.38 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

EC Number Organism UniProt Comment Textmining
3.4.23.38 Plasmodium falciparum P39898
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
3.4.23.38 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)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.23.38 Leu-Glu-Arg-Ile-Phe-(p-nitro)Phe-Ser-Phe + H2O
-
 Plasmodium falciparum Leu-Glu-Arg-Ile-Phe + (p-nitro)Phe-Ser-Phe
-
 ?
3.4.23.38 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
-
 ?
3.4.23.38 Lys-Pro-Ile-Leu-Phe-(p-nitro)Phe-Arg-Leu + H2O
-
 Plasmodium falciparum Lys-Pro-Ile-Leu-Phe + (p-nitro)Phe-Arg-Leu
-
 ?
3.4.23.38 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]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.23.38 1.1
-
 Lys-Pro-Ile-Leu-Phe-(p-nitro)Phe-Arg-Leu pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
3.4.23.38 2.6
-
 Leu-Glu-Arg-Ile-Phe-(p-nitro)Phe-Ser-Phe pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
3.4.23.38 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

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.23.38 4.5
-
 recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.23.38 0.0000014
-
 pepstatin A pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
3.4.23.38 0.0000014
-
 Ro40-4388 pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
3.4.23.38 0.000043
-
 KPFSL-PSI(CH2-NH)-LQF pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
3.4.23.38 0.000073
-
 KPnorLSnorL-PSI(CH2-NH)-LQI pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
3.4.23.38 0.0055
-
 KPLEF-PSI(CH2-NH)-FRV pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
3.4.23.38 0.031
-
 KPVEF-PSI(CH2-NH)-RQT pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
3.4.23.38 0.038
-
 KPLEF-PSI(CH2-NH)-YRV pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum
3.4.23.38 0.042
-
 KPFEL-PSI(CH2-NH)-AWT pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant Plasmodium falciparum