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Literature summary extracted from

  • Affleck, J.G.; Al-Batayneh, K.M.; Neumann, K.; Cole, S.P.; Walker, V.K.
    Drosophila dihydrofolate reductase mutations confer antifolate resistance to mammalian cells (2006), Eur. J. Pharmacol., 529, 71-78.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
1.5.1.3 I26N/K31P less than 10% of wild-type activity Drosophila melanogaster
1.5.1.3 K31P no detectable activity Drosophila melanogaster
1.5.1.3 L22R mutation predicted in silico to be resistant to methotrexate, confers resistance to methotrexate to transfected CHO cells. 65% of wild-type enzyme activity Drosophila melanogaster
1.5.1.3 L30Q mutation found in a methotrexate resistant cell line, confers resistance to methotrexate to transfected CHO cells. 42% of wild-type enzyme activity Drosophila melanogaster
1.5.1.3 Q134K 51% of wild-type enzyme activity Drosophila melanogaster

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 methotrexate wild-type, 50% inhibition at 1.06 nM, mutant Q134K, 50% inhibition at 16.7 nM, mutant L30Q, 50% inhibition at 785 nM Drosophila melanogaster

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.5.1.3 0.00004
-
 7,8-dihydrofolate mutant Q134K, pH 8.5, 25°C Drosophila melanogaster
1.5.1.3 0.00119
-
 7,8-dihydrofolate wild-type, pH 8.5, 25°C Drosophila melanogaster
1.5.1.3 0.0055
-
 NADPH mutant Q134K, pH 8.5, 25°C Drosophila melanogaster
1.5.1.3 0.00592
-
 7,8-dihydrofolate mutant L30Q, pH 8.5, 25°C Drosophila melanogaster
1.5.1.3 0.0069
-
 NADPH wild-type, pH 8.5, 25°C Drosophila melanogaster
1.5.1.3 0.0071
-
 NADPH mutant L30Q, pH 8.5, 25°C Drosophila melanogaster

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Drosophila melanogaster P17719 expression in Chinese hamster ovary cells
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.5.1.3 7,8-dihydrofolate + NADPH
-
 Drosophila melanogaster 5,6,7,8-tetrahydrofolate + NADP+
-
 ?

Cofactor

EC Number Cofactor Comment Organism Structure
1.5.1.3 NADPH
-
 Drosophila melanogaster