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Literature summary for 2.4.2.3 extracted from

  • Renck, D.; Ducati, R.G.; Palma, M.S.; Santos, D.S.; Basso, L.A.
    The kinetic mechanism of human uridine phosphorylase 1: Towards the development of enzyme inhibitors for cancer chemotherapy (2010), Arch. Biochem. Biophys., 497, 35-42.
    View publication on PubMed

Application

Application Comment Organism
drug development UP12 is a target for development of enzyme inhibitors for cancer chemotherapy, design of inhibitors is intended to boost endogenous uridine levels to rescue normal tissues from the toxicity of fluoropyrimidine nucleoside chemotherapeutic agents, such as capecitabine and 5-fluorouracil. Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of UP1 in Escherichia coli strain Rosetta (DE3) Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
alpha-D-ribose 1-phosphate product inhibition pattern, noncompetitive versus uridine, competitive versus phosphate, overview Homo sapiens
Uracil product inhibition pattern, noncompetitive versus uridine and phosphate, overview Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information steady-state kinetics Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
uridine + phosphate Homo sapiens
-
uracil + alpha-D-ribose 1-phosphate
-
r

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16831 UP1; type 1 enzyme
-

Purification (Commentary)

Purification (Comment) Organism
recombinant UP1 3.8fold from Escherichia coli strain Rosetta (DE3) Homo sapiens

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
7.7
-
purified recombinant enzyme Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
uridine + phosphate
-
Homo sapiens uracil + alpha-D-ribose 1-phosphate
-
r

Synonyms

Synonyms Comment Organism
UP type 1
-
Homo sapiens
UP1
-
Homo sapiens
uridine phosphorylase 1
-
Homo sapiens

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
7.6
-
recombinant enzyme Homo sapiens

pH Range

pH Minimum pH Maximum Comment Organism
5 9 recombinant enzyme,m pH profile, overview Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.034
-
alpha-D-ribose 1-phosphate pH 7.4, 37°C, versus uridine Homo sapiens
0.05
-
Uracil pH 7.4, 37°C, versus uridine Homo sapiens
0.137
-
Uracil pH 7.4, 37°C, versus phosphate Homo sapiens
0.494
-
alpha-D-ribose 1-phosphate pH 7.4, 37°C, versus phosphate Homo sapiens

General Information

General Information Comment Organism
metabolism uridine phosphorylase is a key enzyme in the pyrimidine salvage pathway, catalyzing the reversible phosphorolysis of uridine to uracil and ribose-1-phosphate Homo sapiens