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Literature summary for 2.1.2.3 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
Search for more literature for 2.1.2.3

Application

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

Cloned(Commentary)

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

Crystallization (Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
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
Acid Yellow 17 IC50: 0.012 mM Gallus gallus
NCI324571-C IC50: 0.042 mM Gallus gallus
NCI324572-F IC50: 0.012 mM Gallus gallus
NCI3262203-A IC50: 0.012 mM Gallus gallus
NCI47729-M IC50: 0.003 mM Gallus gallus
SALOR2 IC50: 0.0014 mM Gallus gallus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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
-
 ?
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

Organism UniProt Comment Textmining
Gallus gallus P31335
-
-
Homo sapiens P31939
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide
-
 Gallus gallus tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
 ?
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide
-
 Homo sapiens tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
 ?
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
-
 ?
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

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

Cofactor

Cofactor Comment Organism Structure
10-formyltetrahydrofolate
-
 Gallus gallus
10-formyltetrahydrofolate
-
 Homo sapiens

Ki Value [mM]

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0014
-
 IC50: 0.0014 mM Gallus gallus SALOR2
0.003
-
 IC50: 0.003 mM Gallus gallus NCI47729-M
0.012
-
 IC50: 0.012 mM Gallus gallus NCI3262203-A
0.012
-
 IC50: 0.012 mM Gallus gallus NCI324572-F
0.012
-
 IC50: 0.012 mM Gallus gallus Acid Yellow 17
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
0.042
-
 IC50: 0.042 mM Gallus gallus NCI324571-C