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Literature summary for 1.5.1.3 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
Search for more literature for 1.5.1.3

Protein Variants

Protein Variants Comment Organism
I26N/K31P less than 10% of wild-type activity Drosophila melanogaster
K31P no detectable activity Drosophila melanogaster
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
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
Q134K 51% of wild-type enzyme activity Drosophila melanogaster

Inhibitors

Inhibitors Comment Organism Structure
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]

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

Organism

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

Substrates and Products (Substrate)

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

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Drosophila melanogaster