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Literature summary for 2.4.2.1 extracted from

  • Parker, W.B.; Allan, P.W.; Ealick, S.E.; Sorscher, E.J.; Hassan, A.E.; Silamkoti, A.V.; Fowler, A.T.; Waud, W.R.; Secrist, J.A.
    Design and evaluation of 5-modified nucleoside analogs as prodrugs for an E. coli purine nucleoside phosphorylase mutant (2005), Nucleosides Nucleotides Nucleic Acids, 24, 387-392.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
M64V mutant enzyme is able to cleave numerous 5’-modified nucleoside analogs with much greater efficiency than the wild-type enzyme Escherichia coli
M64V naturally occuring mutant, the mutant enzyme is able to cleave numerous 5’-modified nucleoside analogs with much greater efficiency than the wild-type enzyme Escherichia coli

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2-fluoro-2-deoxyadenosine + phosphate Escherichia coli a toxic prodrug ?
-
?
9-[2-deoxy-beta-D-ribofuranosyl]-6-methylpurine + phosphate Escherichia coli a toxic prodrug ?
-
?
9-[6-deoxy-beta-L-talofuranosyl]-2-fluoro-adenine + phosphate Escherichia coli a toxic prodrug, substrate of enzyme mutant M64V, the drug product has anti-tumor activity ?
-
?
9-[6-deoxy-beta-L-talofuranosyl]-6-methylpurine + phosphate Escherichia coli a toxic prodrug, substrate of enzyme mutant M64V, the drug product has anti-tumor activity ?
-
?
9-[beta-D-arabinofuranosyl]-2-fluoro-adenine + phosphate Escherichia coli a toxic prodrug ?
-
?
9-[beta-L-lyxofuranosyl]-2-fluoro-adenine + phosphate Escherichia coli a toxic prodrug, substrate of enzyme mutant M64V, the drug product has anti-tumor activity ?
-
?

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Escherichia coli
-
mutant enzyme M64V
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.015
-
wild-type enzyme, substrate 9-[6-deoxy-beta-L-talofuranosyl]-6-methylpurine Escherichia coli
0.0167
-
mutant M64V, substrate 9-[beta-D-arabinofuranosyl]-2-fluoro-adenine Escherichia coli
0.02
-
wild-type enzyme, substrate 9-[beta-D-arabinofuranosyl]-2-fluoro-adenine Escherichia coli
0.13
-
wild-type enzyme, substrate 9-[6-deoxy-beta-L-talofuranosyl]-2-fluoro-adenine Escherichia coli
0.567
-
wild-type enzyme, substrate 9-[2-deoxy-beta-D-ribofuranosyl]-6-methylpurine Escherichia coli
1.43
-
mutant M64V, substrate 9-[6-deoxy-beta-L-talofuranosyl]-6-methylpurine Escherichia coli
4
-
mutant M64V, substrate 9-[6-deoxy-beta-L-talofuranosyl]-2-fluoro-adenine Escherichia coli
7.3
-
wild-type enzyme, substrate 2-fluoro-2'-deoxyadenosine Escherichia coli
8.83
-
wild-type enzyme, substrate 9-[2-deoxy-beta-D-ribofuranosyl]-6-methylpurine Escherichia coli
9.83
-
mutant M64V, substrate 9-[2-deoxy-beta-D-ribofuranosyl]-6-methylpurine Escherichia coli
23.3
-
mutant M64V, substrate 9-[2-deoxy-beta-D-ribofuranosyl]-6-methylpurine Escherichia coli
26.67
-
mutant M64V, substrate 2-fluoro-2'-deoxyadenosine Escherichia coli

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-fluoro-2-deoxyadenosine + phosphate a toxic prodrug Escherichia coli ?
-
?
9-[2-deoxy-beta-D-ribofuranosyl]-6-methylpurine + phosphate a toxic prodrug Escherichia coli ?
-
?
9-[6-deoxy-alpha-L-talofuranosyl]-2-F-adenine + phosphate
-
Escherichia coli ?
-
?
9-[6-deoxy-alpha-L-talofuranosyl]-6-methylpurine + phosphate
-
Escherichia coli ?
-
?
9-[6-deoxy-beta-L-talofuranosyl]-2-fluoro-adenine + phosphate a toxic prodrug, substrate of enzyme mutant M64V, the drug product has anti-tumor activity Escherichia coli ?
-
?
9-[6-deoxy-beta-L-talofuranosyl]-2-fluoro-adenine + phosphate a toxic prodrug, substrate of enzyme mutant M64V Escherichia coli ?
-
?
9-[6-deoxy-beta-L-talofuranosyl]-6-methylpurine + phosphate a toxic prodrug, substrate of enzyme mutant M64V, the drug product has anti-tumor activity Escherichia coli ?
-
?
9-[6-deoxy-beta-L-talofuranosyl]-6-methylpurine + phosphate a toxic prodrug, substrate of enzyme mutant M64V, liberation of methylpurine Escherichia coli ?
-
?
9-[alpha-L-lyxofuranosyl]-2-F-adenine + phosphate
-
Escherichia coli ?
-
?
9-[beta-D-arabinofuranosyl]-2-fluoro-adenine + phosphate a toxic prodrug Escherichia coli ?
-
?
9-[beta-L-lyxofuranosyl]-2-fluoro-adenine + phosphate a toxic prodrug, substrate of enzyme mutant M64V, the drug product has anti-tumor activity Escherichia coli ?
-
?
9-[beta-L-lyxofuranosyl]-2-fluoro-adenine + phosphate a toxic prodrug, substrate of enzyme mutant M64V Escherichia coli ?
-
?

Synonyms

Synonyms Comment Organism
purine nucleoside phosphorylase
-
Escherichia coli