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Literature summary for 2.1.2.3 extracted from

  • Wall, M.; Shim, J.H.; Benkovic, S.J.
    Human AICAR transformylase: Role of the 4-Carboxamide of AICAR in binding and catalysis (2000), Biochemistry, 39, 11303-11311.
    View publication on PubMed

Application

Application Comment Organism
medicine target for development of inhibitors with potential use as chemotherapeutic agents Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-N-allyl-5-aminoimidazole-4-carboxamide ribonucleotide
-
Homo sapiens
4-N-methyl-5-aminoimidazole-4-carboxamide ribonucleotide
-
Homo sapiens
5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide product inhibitor Homo sapiens
5-amino-1-beta-D-ribofuranosylimidazole 5'-phosphate
-
Homo sapiens
5-amino-1-beta-D-ribofuranosylimidazole-4-carbonitrile 5'-phosphate
-
Homo sapiens
5-amino-1-beta-D-ribofuranosylimidazole-4-carboxamidoxime 5'-phosphate
-
Homo sapiens
5-amino-1-beta-D-ribofuranosylimidazole-4-carboxylate 5'-phosphate
-
Homo sapiens
5-amino-4-nitro-1-beta-D-ribofuranosylimidazole 5'-phosphate
-
Homo sapiens
5-formyl-5-aminoimidazole-4-carboxamide ribonucleotide
-
Homo sapiens
AMP
-
Homo sapiens
XMP
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0009
-
5-amino-imidazole-4-thiocarboxamide ribonucleotide 10-formyldihydrofolate as cofactor Homo sapiens
0.0015
-
5-aminoimidazole-4-carboxamide ribonucleotide 10-formyldihydrofolate as cofactor Homo sapiens
0.0019
-
5-aminoimidazole-4-carboxamide ribonucleotide 10-formyltetrahydrofolate as cofactor Homo sapiens
0.01
-
5-aminoimidazole-4-carboxamide ribonucleotide
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide Escherichia coli
-
tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide Homo sapiens
-
tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Homo sapiens
-
human
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide
-
Escherichia coli tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide
-
Homo sapiens tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
10-formyltetrahydrofolate + 5-amino-imidazole-4-thiocarboxamide ribonucleotide
-
Homo sapiens tetrahydrofolate + 6-mercaptopurine ribonucleotide
-
?
additional information in all organisms studied to date AICARFT activity is accompanied by inosine monophosphate cyclohydrolase located on the same polypeptide encoded by the purH gene Escherichia coli ?
-
?
additional information in all organisms studied to date AICARFT activity is accompanied by inosine monophosphate cyclohydrolase located on the same polypeptide encoded by the purH gene Homo sapiens ?
-
?
N10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide
-
Escherichia coli tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide
-
r
N10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide
-
Homo sapiens tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide
-
r

Cofactor

Cofactor Comment Organism Structure
10-formyldihydrofolate
-
Homo sapiens
10-formylfolate
-
Homo sapiens
N10-formyltetrahydrofolate
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0004
-
5-formyl-5-aminoimidazole-4-carboxamide ribonucleotide
-
Homo sapiens
0.0007
-
5-amino-4-nitroimidazole ribonucleotide
-
Homo sapiens
0.0007
-
5-amino-4-nitro-1-beta-D-ribofuranosylimidazole 5'-phosphate
-
Homo sapiens
0.0012
-
XMP
-
Homo sapiens
0.006
-
5-amino-1-beta-D-ribofuranosylimidazole 5'-phosphate
-
Homo sapiens
0.01
-
5-amino-1-beta-D-ribofuranosylimidazole-4-carboxylate 5'-phosphate
-
Homo sapiens
0.026
-
5-amino-1-beta-D-ribofuranosylimidazole-4-carbonitrile 5'-phosphate
-
Homo sapiens
0.027
-
AMP
-
Homo sapiens