Application | Comment | Organism |
---|---|---|
medicine | use of thymidine phosphorylase inhibitors might offer a promising strategy for cancer treatment | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D203A | site-directed mutagenesis, the mutant enzyme shows 50fold reduced catalytic efficiency compared to the wild-type enzyme, the mutant also shows pronounced resistance to the inhibitory effect of 5'-O-tritylinosine, and it keeps full sensitivity to the competitive inhibitors 6-aminothymine and 6-amino-5-bromouracil | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
5'-O-tritylinosine | i.e. KIN59, noncompetitive. Inhibitor docking and conformational changes, molecular modeling using the crystal structure of the enzyme, molecular dynamics simulations, binding site and mode, overview | Homo sapiens | |
6-amino-5-bromouracil | - |
Homo sapiens | |
6-aminothymine | - |
Homo sapiens | |
7-deazaxanthine | - |
Homo sapiens | |
9-[8-phosphonooctyl]-7-deazaxanthine | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.414 | - |
thymine | pH 7.6, wild-type enzyme | Homo sapiens | |
9.828 | - |
thymine | pH 7.6, mutant D203A | Homo sapiens |
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 |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P19971 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
carcinoma cell | the enzyme is upregulated in many solid tumors | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
thymidine + phosphate | - |
Homo sapiens | thymine + 2-deoxy-alpha-D-ribose 1-phosphate | - |
r | |
thymidine + phosphate | Asp203 plays an important role to afford the substrate-binding site loop stabilization that is required for efficient enzyme catalysis | Homo sapiens | thymine + 2-deoxy-alpha-D-ribose 1-phosphate | - |
r |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.6 | - |
assay at | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
metabolism | thymidine phosphorylase is a catabolic enzyme in thymidine metabolism | Homo sapiens |
additional information | elevated enzyme levels are associated with tumor angiogenesis, metastasis and poor prognosis | Homo sapiens |