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Literature summary for 2.4.2.4 extracted from

  • Oh, T.; El Kouni, M.H.
    Kinetics mechanism and regulation of native human hepatic thymidine phosphorylase (2019), Int. J. Biochem. Cell Biol., 110, 122-129 .
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
2-deoxy-alpha-D-ribose 1-phosphate dRib-1-P , a noncompetitive product inhibitor of the forward reaction, in the reverse reaction, dRib-1-P enhanced the binding of thymine Homo sapiens
thymine thymine is a product activator, but becomes a substrate inhibitor at concentrations eight times higher than its Km. Competitive substrate inhibition at high concentration for the human liver TP Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-deoxy-alpha-D-ribose 1-phosphate dRib-1-P , a non-competitive product inhibitor of the forward reaction, in the reverse reaction, dRib-1-P enhanced the binding of thymine Homo sapiens
2-deoxy-alpha-D-ribose 1-phosphate dRib-1-P is a competitive product inhibitor of the forward reaction, in the reverse reaction, dRib-1-P enhances the binding of thymine Mus musculus
thymidine yields a non-competitive inhibition pattern in agreement with a random mechanism Homo sapiens
thymine thymine is a product activator, but becomes a substrate inhibitor at concentrations eight times higher than its Km. Thymine is an effector rather than a product inhibitor Homo sapiens
thymine thymine is a product activator, but becomes a competitive inhibitor at concentrations eight times higher than its Km Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetic mechanism and regulation of native human hepatic thymidine phosphorylase (TP), kinetics Homo sapiens
0.0058
-
phosphate pH 7.5, 37°C Homo sapiens
0.09
-
2-deoxy-alpha-D-ribose 1-phosphate pH 7.5, 37°C Homo sapiens
0.244
-
thymine pH 7.5, 37°C Homo sapiens
0.284
-
thymidine pH 7.5, 37°C Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P19971
-
-
Mus musculus Q99N42
-
-

Reaction

Reaction Comment Organism Reaction ID
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate sequential random bi-bi mechanism Homo sapiens
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate sequential random bi-bi mechanism Mus musculus

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information initial velocity studies showed an intersecting pattern, consistent with substrate-enzyme-co-substrate complex formation, and a binding pattern indicating that the binding of the substrate interferes with the binding of the co-substrate and vice versa Homo sapiens ?
-
-
thymidine + phosphate
-
Homo sapiens thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
r
thymidine + phosphate
-
Mus musculus thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
r
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Homo sapiens thymidine + phosphate
-
r
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Mus musculus thymidine + phosphate
-
r

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5 8.5 thymidine phosphorolysis Homo sapiens
7.5
-
thymidine synthesis Homo sapiens

pH Range

pH Minimum pH Maximum Comment Organism
5 9 activity range of synthesis of thymidine, profile overview Homo sapiens
5 11 activity range of phosphorolysis of thymidine, profile overview Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics Homo sapiens
additional information
-
additional information inhibition kinetics Mus musculus

General Information

General Information Comment Organism
physiological function thymidine phosphorylase (TP) catalyzes the reversible phosphorolysis of thymidine, deoxyuridine, and their analogues to their respective nucleobases and 2-deoxy-alpha-D-ribose-1-phosphate. TP is a key enzyme in the pyrimidine salvage pathways. Activity of the enzyme is crucial in angiogenesis, cancer chemotherapy, radiotherapy, and tumor imaging Homo sapiens