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Literature summary extracted from

  • Afshar, S.; Olafsen, T.; Wu, A.; Morrison, S.
    Characterization of an engineered human purine nucleoside phosphorylase fused to an anti-her2/neu single chain Fv for use in ADEPT (2009), J. Exp. Clin. Cancer Res., 28, 147.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.4.2.1 medicine use of mutant E201Q/N243D in Antibody Dependent Enzyme Prodrug Therapy ADEPT by fusion to the human anti-HER2/neu single chain Fv. In vitro the construct binds specifically to HER2/neu expressing tumor cells and localizes the enzyme to tumor cells, where the enzymatic activity of the mutant, but not the wild type enzyme, results in phosphorolysis of the prodrug, 2-fluoro-2'-deoxyadenosine to the cytotoxic drug 2-fluoroadenine causing inhibition of tumor cell proliferation Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.4.2.1 E201Q/N243D unlike wild-type, mutant is able to cleave prodrugs 2-fluoro-2'-deoxyadenosine, Cladribine, and 2-fluoroadenosine Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.2.1 0.059
-
 guanosine mutant E201Q/N243D Homo sapiens
2.4.2.1 0.264
-
 2-fluoro-2'-deoxyadenosine mutant E201Q/N243D Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.1 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.1 2-fluoro-2-deoxyadenosine + phosphate no substrate for wild-type, substrate of double mutant E201Q/N243D Homo sapiens adenine + 2-fluoro-2-deoxy-alpha-D-ribose 1-phosphate
-
 ?
2.4.2.1 guanosine + phosphate
-
 Homo sapiens guanine + alpha-D-ribose 1-phosphate
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.4.2.1 0.155
-
 2-fluoro-2'-deoxyadenosine mutant E201Q/N243D Homo sapiens
2.4.2.1 60
-
 guanosine mutant E201Q/N243D Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
2.4.2.1 568
-
 2-fluoro-2'-deoxyadenosine mutant E201Q/N243D Homo sapiens
2.4.2.1 1020
-
 guanosine mutant E201Q/N243D Homo sapiens