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Literature summary extracted from

  • Xu, L.; Li, C.; Olson, A.J.; Wilson, I.A.
    Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate inhibitor identified by virtual ligand screening (2004), J. Biol. Chem., 279, 50555-50565.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.1.2.3 medicine potential target for antineoplastic chemotherapy Gallus gallus
2.1.2.3 medicine potential target for antineoplastic chemotherapy Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.1.2.3 expressed in Escherichia coli BL21.DE3 as His-tag fusion protein Gallus gallus
2.1.2.3 expressed in Escherichia coli BL21.DE3 as His-tag fusion protein Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.1.2.3 crystallized in complex with its inhibitor 2-[5-hydroxy-3-methyl-1-(2-methyl-4-sulfophenyl)-1H-pyrazo]-4-sulfobenzoic acid Gallus gallus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.2.3 2-[5-hydroxy-3-methyl-1-(2-methyl-4-sulfophenyl)-1H-pyrazo]-4-sulfobenzoic acid Acid Yellow 54, 326203-A, competitive against 10-formyltetrahydrofolate, IC50: 0.012 mM, inhibitor partially blocks the cofactor binding site Gallus gallus
2.1.2.3 Acid Yellow 17 IC50: 0.012 mM Gallus gallus
2.1.2.3 NCI324571-C IC50: 0.042 mM Gallus gallus
2.1.2.3 NCI324572-F IC50: 0.012 mM Gallus gallus
2.1.2.3 NCI3262203-A IC50: 0.012 mM Gallus gallus
2.1.2.3 NCI47729-M IC50: 0.003 mM Gallus gallus
2.1.2.3 SALOR2 IC50: 0.0014 mM Gallus gallus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide Gallus gallus penultimate step of the purine de novo synthesis pathway tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide Homo sapiens penultimate step of the purine de novo synthesis pathway tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.1.2.3 Gallus gallus P31335
-
-
2.1.2.3 Homo sapiens P31939
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.1.2.3 recombinant protein using His-tag Gallus gallus
2.1.2.3 recombinant protein using His-tag Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide
-
Gallus gallus tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide
-
Homo sapiens tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide penultimate step of the purine de novo synthesis pathway Gallus gallus tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide penultimate step of the purine de novo synthesis pathway Homo sapiens tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?

Synonyms

EC Number Synonyms Comment Organism
2.1.2.3 AICAR transformylase/inosine monophosphate cyclohydrolase bifunctional enzyme catalyzing the last two steps of the purine de novo synthesis pathway Gallus gallus
2.1.2.3 AICAR transformylase/inosine monophosphate cyclohydrolase bifunctional enzyme catalyzing the last two steps of the purine de novo synthesis pathway Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.1.2.3 10-formyltetrahydrofolate
-
Gallus gallus
2.1.2.3 10-formyltetrahydrofolate
-
Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.2.3 0.007
-
2-[5-hydroxy-3-methyl-1-(2-methyl-4-sulfophenyl)-1H-pyrazo]-4-sulfobenzoic acid pH 7.5 Gallus gallus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.1.2.3 0.0014
-
IC50: 0.0014 mM Gallus gallus SALOR2
2.1.2.3 0.003
-
IC50: 0.003 mM Gallus gallus NCI47729-M
2.1.2.3 0.012
-
IC50: 0.012 mM Gallus gallus NCI3262203-A
2.1.2.3 0.012
-
IC50: 0.012 mM Gallus gallus NCI324572-F
2.1.2.3 0.012
-
IC50: 0.012 mM Gallus gallus Acid Yellow 17
2.1.2.3 0.012
-
Acid Yellow 54, 326203-A, competitive against 10-formyltetrahydrofolate, IC50: 0.012 mM, inhibitor partially blocks the cofactor binding site Gallus gallus 2-[5-hydroxy-3-methyl-1-(2-methyl-4-sulfophenyl)-1H-pyrazo]-4-sulfobenzoic acid
2.1.2.3 0.042
-
IC50: 0.042 mM Gallus gallus NCI324571-C