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Literature summary for 2.4.2.4 extracted from

  • Liekens, S.; Bronckaers, A.; Perez-Perez, M.J.; Balzarini, J.
    Targeting platelet-derived endothelial cell growth factor/thymidine phosphorylase for cancer therapy (2007), Biochem. Pharmacol., 74, 1555-1567.
    View publication on PubMed
Search for more literature for 2.4.2.4

Activating Compound

Activating Compound Comment Organism Structure
cyclophosphamide induces thymidine phosphorylase expression Homo sapiens
docetaxel induces thymidine phosphorylase expression Homo sapiens
interferon alpha causes a rapid and transient increase of thymidine phosphorylase expression Homo sapiens
interferon beta causes a rapid and transient increase of thymidine phosphorylase expression Homo sapiens
interferon gamma causes a rapid and transient increase of thymidine phosphorylase expression Homo sapiens
interleukin-1beta the expression of tyhmidine phosphorylase mRNA is significantly increased by stimulation with interleukin-1beta Homo sapiens
mitomycin C induces thymidine phosphorylase expression Homo sapiens
additional information the enzymatic activity of thymidine phosphorylase is required for the activation of 5-fluorouracil prodrugs, the enzyme induces the expression of several matrix metalloproteinases, increases the levels of hypoxia-inducible factor 1alpha during in vitro hypoxia Homo sapiens
paclitaxel induces thymidine phosphorylase expression Homo sapiens
Tumor necrosis factor alpha causes a rapid and transient increase of thymidine phosphorylase expression Homo sapiens

Application

Application Comment Organism
medicine thymidine phosphorylase expression correlates well with tumor grade, metastasis and shorter patient survival in colorectal, pancreatic, renal, ovarian, cervical, bladder and non-small cell lung cancer, loss of function mutants of thymidine phosphorylase case the disease mitochondrial neurogastrointestinal encephalomyopathy Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
-
 Homo sapiens

Protein Variants

Protein Variants Comment Organism
L148R mutant devoid of enzymatic activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5'-O-tritylinosine
-
 Homo sapiens
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracil hydrochloride
-
 Homo sapiens
6-amino-5-bromouracil
-
 Homo sapiens
6-amino-5-chlorouracil
-
 Homo sapiens
6-aminothymine
-
 Homo sapiens
aurothioglucose the expression of tyhmidine phosphorylase mRNA is significantly decreased by stimulation with aurothioglucose Homo sapiens
dexamethasone the expression of tyhmidine phosphorylase mRNA is significantly decreased by stimulation with dexamethasone Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-431 cell
-
 Homo sapiens
-
colonic cancer cell
-
 Homo sapiens
-
gastrointestinal tract high expression Homo sapiens
-
HT-29 cell
-
 Homo sapiens
-
KK-47 cell
-
 Homo sapiens
-
MKN-74 cell
-
 Homo sapiens
-
prostate cancer cell
-
 Homo sapiens
-
RT-112 cell
-
 Homo sapiens
-
THP-1 cell
-
 Homo sapiens
-
U-937 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5'-deoxy-5-fluorouridine + phosphate
-
 Homo sapiens 5-fluorouracil + 5-deoxyribose-1-phosphate
-
 ?
5-fluoro-2'-deoxyuridine + phosphate
-
 Homo sapiens 5-fluorouracil + 2-deoxyribose-1-phosphate
-
 r
thymidine + phosphate
-
 Homo sapiens thymine + 2-deoxy-D-ribose 1-phosphate
-
 ?

Subunits

Subunits Comment Organism
dimer x-ray crystallography Homo sapiens

Synonyms

Synonyms Comment Organism
gliostatin
-
 Homo sapiens
PD-ECGF
-
 Homo sapiens
platelet-derived endothelial cell growth factor
-
 Homo sapiens