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Literature summary for 2.4.2.1 extracted from

  • Todorova, N.A.; Schwarz, F.P.
    Effect of the phosphate substrate on drug-inhibitor binding to human purine nucleoside phosphorylase (2008), Arch. Biochem. Biophys., 480, 122-131.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
9-benzylguanine isothermal titration calorimetry study. At 25°C, the tighter 9-benzylguanine binding reaction goes from an enthalpically-driven reaction in the absence of phosphate to an entropically-driven reaction at 10 mM phosphate, and the enthalpically-driven nature of the binding reaction is restored at 75 mM phosphate. Bound phosphate affects the interactions of the side-chains with the ribose catalytic site. 9-Benzylguanine interacts with Phe159 from an adjacent subunit Homo sapiens
acyclovir isothermal titration calorimetry study. At 25°C and with an increase in the phosphate concentration from 0 to 50 mM, acyclovir binding becomes more entropically-driven Homo sapiens
ganciclovir isothermal titration calorimetry study. At 25°C and with an increase in the phosphate concentration from 0 to 50 mM, ganciclovir binding becomes more enthalpically-driven Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
9.2
-
7-methylguanosine presence of 50 mM phosphate, pH 7.0 Homo sapiens
12.5
-
7-methylguanosine presence of 50 mM phosphate, pH 7.0 Homo sapiens
13
-
7-methylguanosine presence of 100 mM phosphate, pH 7.0 Homo sapiens
13.9
-
7-methylguanosine presence of 100 mM phosphate, pH 7.0 Homo sapiens
16.3
-
7-methylguanosine presence of 100 mM phosphate, pH 7.0 Homo sapiens
39.3
-
7-methylguanosine presence of 50 mM phosphate, pH 7.0 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
12
-
presence of 100 mM phosphate, pH 7.0 Homo sapiens
20
-
presence of 50 mM phosphate, pH 7.0 Homo sapiens
41
-
presence of 50 mM phosphate, pH 7.0 Homo sapiens
46
-
presence of 100 mM phosphate, pH 7.0 Homo sapiens
47
-
presence of 100 mM phosphate, pH 7.0 Homo sapiens
139
-
presence of 50 mM phosphate, pH 7.0 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7-methylguanosine + phosphate
-
Homo sapiens 7-methylguanine + alpha-D-ribose 1-phosphate
-
?

Subunits

Subunits Comment Organism
monomer partial dissociation of the purine nucleotide phosphates trimer into monomers below 60 nM Homo sapiens
trimer partial dissociation of the purine nucleotide phosphates trimer into monomers below 60 nM Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
6.23
-
7-methylguanosine presence of 100 mM phosphate, pH 7.0 Homo sapiens
9.2
-
7-methylguanosine presence of 50 mM phosphate, pH 7.0 Homo sapiens
20.4
-
7-methylguanosine presence of 50 mM phosphate, pH 7.0 Homo sapiens
23
-
7-methylguanosine presence of 100 mM phosphate, pH 7.0 Homo sapiens
24.7
-
7-methylguanosine presence of 100 mM phosphate, pH 7.0 Homo sapiens
73.1
-
7-methylguanosine presence of 50 mM phosphate, pH 7.0 Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
240
-
7-methylguanosine presence of 50 mM phosphate, pH 7.0 Homo sapiens
488
-
7-methylguanosine presence of 100 mM phosphate, pH 7.0 Homo sapiens
1548
-
7-methylguanosine presence of 100 mM phosphate, pH 7.0 Homo sapiens
1674
-
7-methylguanosine presence of 100 mM phosphate, pH 7.0 Homo sapiens
2256
-
7-methylguanosine presence of 50 mM phosphate, pH 7.0 Homo sapiens
5860
-
7-methylguanosine presence of 50 mM phosphate, pH 7.0 Homo sapiens