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Literature summary for 1.5.1.3 extracted from

  • Roth, B.; Bliss, E.; Beddell, C.R.
    Inhibitors of dihydrofolate reductase (1983), Top. Mol. Struct. Biol., 3, 363-393.
No PubMed abstract available

Application

Application Comment Organism
medicine enzyme is a target of several anti-folate inhibitory drugs to combat bacteria, protozoa and cancer Gallus gallus
medicine enzyme is a target of several anti-folate inhibitory drugs to combat bacteria, protozoa and cancer Escherichia coli
medicine enzyme is a target of several anti-folate inhibitory drugs to combat bacteria, protozoa and cancer Homo sapiens
medicine enzyme is a target of several anti-folate inhibitory drugs to combat bacteria, protozoa and cancer Sus scrofa
medicine enzyme is a target of several anti-folate inhibitory drugs to combat bacteria, protozoa and cancer Bos taurus
medicine enzyme is a target of several anti-folate inhibitory drugs to combat bacteria, protozoa and cancer Lacticaseibacillus casei
medicine enzyme is a target of several anti-folate inhibitory drugs to combat bacteria, protozoa and cancer Enterococcus faecium

Crystallization (Commentary)

Crystallization (Comment) Organism
crystal structure, complex with 2,4-diamino-5,6-dihydro-6,6-dimethyl-5-(4'-methoxyphenyl)-s-triazine Gallus gallus
structure of ternary complex with NADPH and methotrexate Escherichia coli
structure of ternary complex with NADPH and methotrexate Lacticaseibacillus casei

Inhibitors

Inhibitors Comment Organism Structure
2,4-diamino-5,6-dihydro-6,6-dimethyl-5-(4'-methoxyphenyl)-s-triazine
-
Gallus gallus
methotrexate
-
Bos taurus
methotrexate dihydrofolate antagonist drug Escherichia coli
methotrexate
-
Gallus gallus
methotrexate dihydrofolate antagonist drug Homo sapiens
methotrexate
-
Lacticaseibacillus casei
methotrexate
-
Sus scrofa
additional information overview Bos taurus
additional information overview Enterococcus faecium
additional information overview Escherichia coli
additional information overview Gallus gallus
additional information overview Lacticaseibacillus casei
additional information overview Sus scrofa

Organism

Organism UniProt Comment Textmining
Bos taurus
-
overview
-
Enterococcus faecium
-
overview
-
Escherichia coli
-
-
-
Gallus gallus
-
overview
-
Homo sapiens
-
methotrexate-resistant WIL-2 lymphoblastoid cells
-
Lacticaseibacillus casei
-
-
-
Sus scrofa
-
overview
-

Reaction

Reaction Comment Organism Reaction ID
5,6,7,8-tetrahydrofolate + NADP+ = 7,8-dihydrofolate + NADPH + H+ inhibitor binding mechanism Gallus gallus
5,6,7,8-tetrahydrofolate + NADP+ = 7,8-dihydrofolate + NADPH + H+ inhibitor binding mechanism Escherichia coli
5,6,7,8-tetrahydrofolate + NADP+ = 7,8-dihydrofolate + NADPH + H+ inhibitor binding mechanism Homo sapiens
5,6,7,8-tetrahydrofolate + NADP+ = 7,8-dihydrofolate + NADPH + H+ inhibitor binding mechanism Sus scrofa
5,6,7,8-tetrahydrofolate + NADP+ = 7,8-dihydrofolate + NADPH + H+ inhibitor binding mechanism Bos taurus
5,6,7,8-tetrahydrofolate + NADP+ = 7,8-dihydrofolate + NADPH + H+ inhibitor binding mechanism Lacticaseibacillus casei
5,6,7,8-tetrahydrofolate + NADP+ = 7,8-dihydrofolate + NADPH + H+ inhibitor binding mechanism Enterococcus faecium

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7,8-dihydrofolate + NADPH
-
Gallus gallus 5,6,7,8-tetrahydrofolate + NADP+
-
?
7,8-dihydrofolate + NADPH
-
Escherichia coli 5,6,7,8-tetrahydrofolate + NADP+
-
?
7,8-dihydrofolate + NADPH
-
Homo sapiens 5,6,7,8-tetrahydrofolate + NADP+
-
?
7,8-dihydrofolate + NADPH
-
Sus scrofa 5,6,7,8-tetrahydrofolate + NADP+
-
?
7,8-dihydrofolate + NADPH
-
Bos taurus 5,6,7,8-tetrahydrofolate + NADP+
-
?
7,8-dihydrofolate + NADPH
-
Lacticaseibacillus casei 5,6,7,8-tetrahydrofolate + NADP+
-
?
7,8-dihydrofolate + NADPH
-
Enterococcus faecium 5,6,7,8-tetrahydrofolate + NADP+
-
?

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Gallus gallus
NADPH
-
Escherichia coli
NADPH
-
Homo sapiens
NADPH
-
Sus scrofa
NADPH
-
Bos taurus
NADPH
-
Lacticaseibacillus casei
NADPH
-
Enterococcus faecium

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000037
-
2,4-diamino-5,6-dihydro-6,6-dimethyl-5-(4'-methoxyphenyl)-s-triazine
-
Gallus gallus