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Literature summary for 4.3.3.6 extracted from

  • Reeksting, S.; Müller, I.; Burger, P.; Burgos, E.; Salmon, L.; Louw, A.; Birkholtz, L.; Wrenger, C.
    Exploring inhibition of Pdx1, a component of the PLP synthase complex of the human malaria parasite Plasmodium falciparum (2013), Biochem. J., 449, 175-187.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
Strep-Tag-fusion proteins expressed in Escherichia coli BLR (DE3) Plasmodium falciparum

Protein Variants

Protein Variants Comment Organism
D26A/K83A/K151A no formation of an internal chromophore with characteristic absorbance at 320 nm during reaction (observed with wild type protein) Plasmodium falciparum
E136A/R139A/R140A formation of an internal chromophore with characteristic absorbance at 320 nm during reaction (also observed with wild type protein) Plasmodium falciparum
additional information multiple deletion mutant proteins Plasmodium falciparum
R167A reduced formation of an internal chromophore with characteristic absorbance at 320 nm during reaction (observed with wild type protein), 50% wild type activity Plasmodium falciparum
R85A/H88A/E91A no formation of an internal chromophore with characteristic absorbance at 320 nm during reaction (observed with wild type protein), dodecameric assembly prevented Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
2-deoxy-D-ribose 5-phosphate at 12 mM 56% residual activity Plasmodium falciparum
4-phospho-D-erythronhydrazide
-
Plasmodium falciparum
D-erythronhydrazide
-
Plasmodium falciparum
D-erythrose
-
Plasmodium falciparum
D-erythrose 4-phosphate
-
Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Purification (Commentary)

Purification (Comment) Organism
affinity chromatography using the Strep-Tag Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-ribose 5-phosphate + glyceraldehyde 3-phosphate + NH4+
-
Plasmodium falciparum pyridoxal 5'-phosphate + 4 H2O + phosphate
-
?

Synonyms

Synonyms Comment Organism
Pdx1 pyridoxal 5'-phosphate synthase complex consits of Pdx1 and Pdx2 Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.016
-
Pdx1 in the heteromeric pyridoxal 5'-phosphate synthase complex, pH 8.0, 37°C Plasmodium falciparum 4-phospho-D-erythronhydrazide
0.043
-
Pdx1, pH 8.0, 37°C Plasmodium falciparum 4-phospho-D-erythronhydrazide
0.902
-
Pdx1, pH 8.0, 37°C Plasmodium falciparum D-erythronhydrazide
3.7
-
Pdx1, pH 8.0, 37°C Plasmodium falciparum D-erythrose 4-phosphate
160
-
Pdx1, pH 8.0, 37°C Plasmodium falciparum D-erythrose