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Literature summary extracted from

  • Mitsiki, E.; Papageorgiou, A.C.; Iyer, S.; Thiyagarajan, N.; Prior, S.H.; Sleep, D.; Finnis, C.; Acharya, K.R.
    Structures of native human thymidine phosphorylase and in complex with 5-iodouracil (2009), Biochem. Biophys. Res. Commun., 386, 666-670.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.2.4 expression of wild-type and mutan enzymes in Escherichia coli strain BL21(DE3) Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.4.2.4 purified recombinant thymidine phosphorylase, free and in complex with 5-iodouracil, X-ray diffraction structure determination and analysis at 3.0 A and 2.5 A resolutions, respectively Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.4.2.4 H116F site-directed mutagenesis, inactive mutant Homo sapiens
2.4.2.4 H116K site-directed mutagenesis, inactive mutant Homo sapiens
2.4.2.4 I214A site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type enzyme Homo sapiens
2.4.2.4 K115A site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type enzyme Homo sapiens
2.4.2.4 K115E site-directed mutagenesis, inactive mutant Homo sapiens
2.4.2.4 R202E site-directed mutagenesis, inactive mutant Homo sapiens
2.4.2.4 R202S site-directed mutagenesis, inactive mutant Homo sapiens
2.4.2.4 S217G site-directed mutagenesis, inactive mutant Homo sapiens
2.4.2.4 Y199A site-directed mutagenesis, inactive mutant Homo sapiens
2.4.2.4 Y199F site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type enzyme Homo sapiens
2.4.2.4 Y199L site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type enzyme Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.4 5-Iodouracil His116 directly interacts with the inhibitor via its NE2 group, enzyme binding structure, overview Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.2.4 0.35
-
 thymidine ph 5.5, 37°C, recombinant wild-type enzyme Homo sapiens
2.4.2.4 0.42
-
 thymidine ph 5.5, 37°C, recombinant mutant K115A Homo sapiens
2.4.2.4 0.74
-
 thymidine ph 5.5, 37°C, recombinant mutant I214A Homo sapiens
2.4.2.4 2.1
-
 thymidine ph 5.5, 37°C, recombinant mutant Y199F Homo sapiens
2.4.2.4 3.14
-
 thymidine ph 5.5, 37°C, recombinant mutant Y199L Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.2.4 thymidine + phosphate Homo sapiens
-
 thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
 r

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.4 Homo sapiens P19971
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.4.2.4 recombinant wild-type and mutan enzymes from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and gel filtration Homo sapiens

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.4.2.4 additional information
-
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.4 thymidine + phosphate
-
 Homo sapiens thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
 r
2.4.2.4 thymidine + phosphate the enzyme catalyzes the reversible cleavage of the glycosidic bond of pyrimidine 2'-deoxynucleotides, most likely through SN2-like transition state involving nucleobase, 2'-deoxyribose and phosphate. The active site consists of residues His116, Ser117, Leu148, Arg202, Val208, Ile214, Lys221 and Val241 Homo sapiens thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
 r

Synonyms

EC Number Synonyms Comment Organism
2.4.2.4 More the enzyme belongs to the pyrimidine nucleoside phosphorylase family Homo sapiens
2.4.2.4 PDECGF
-
 Homo sapiens
2.4.2.4 platelet derived endothelial cell growth factor
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.2.4 37
-
 assay at Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.4.2.4 3.5
-
 thymidine ph 5.5, 37°C, recombinant mutant Y199F Homo sapiens
2.4.2.4 4.4
-
 thymidine ph 5.5, 37°C, recombinant mutant Y199L Homo sapiens
2.4.2.4 5.2
-
 thymidine ph 5.5, 37°C, recombinant mutant I214A Homo sapiens
2.4.2.4 6.8
-
 thymidine ph 5.5, 37°C, recombinant mutant K115A Homo sapiens
2.4.2.4 8.2
-
 thymidine ph 5.5, 37°C, recombinant wild-type enzyme Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.2.4 5.5
-
 thymine production, assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.2.4 0.48
-
 5-Iodouracil
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
2.4.2.4 metabolism the enzyme plays a key role in nucleoside metabolism Homo sapiens
2.4.2.4 physiological function the enzyme is the sole endothelial mitogenic and angiogenic factor, it plays a role in the stimulation of chemotaxis and thymidine incorporation into endothelial cells in vitro and angiogenesis in vivo Homo sapiens