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Literature summary extracted from

  • Szabados, E.; Hindmarsh, E.J.; Phillips, L.; Duggleby, R.G.; Christopherson, R.I.
    5-Aminoimidazole-4-carboxamide ribotide transformylase-IMP cyclohydrolase from human CCRF-CEM leukemia cells: purification, pH dependence and inhibitors (1994), Biochemistry, 33, 14237-14245.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.1.2.3 medicine
-
Gallus sp.
2.1.2.3 medicine target for development of inhibitors with potential use as chemotherapeutic agents Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.2.3 4-amino-10-methylpteroylglutamic acid methotrexate, non-competitive inhibitor Gallus sp.
2.1.2.3 4-amino-10-methylpteroylglutamic acid methotrexate, non-competitive inhibitor Homo sapiens
2.1.2.3 KCl
-
Homo sapiens
3.5.4.10 2'-deoxy-AMP decreased IMP cyclohydrolase activity by 10-50% Homo sapiens
3.5.4.10 2-fluoroadenine arabinoside 5'-monophosphate IC50-value in cell culture 0.0002 mM; strong competitive inhibitor, derivative of anti-cancer drug Homo sapiens
3.5.4.10 2-mercaptoinosine 5'-monophosphate most potent competitive inhibitor, precursor of GMP in the purine pathway Homo sapiens
3.5.4.10 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside decreased IMP cyclohydrolase activity by 10-50% Homo sapiens
3.5.4.10 6-mercaptopurine riboside 5'-monophosphate IC50-value in cell culture 0.0075 mM; strong competitive inhibitor, derivative of anti-cancer drug Homo sapiens
3.5.4.10 adenosine N1-oxide 5'-monophosphate IC50-value in cell culture 0.0011 microM; strong competitive inhibitor Homo sapiens
3.5.4.10 AMP decreased IMP cyclohydrolase activity by 10-50% Homo sapiens
3.5.4.10 GMP decreased IMP cyclohydrolase activity by 10-50% Homo sapiens
3.5.4.10 IMP decreased IMP cyclohydrolase activity by 10-50% Homo sapiens
3.5.4.10 N-succino-AMP decreased IMP cyclohydrolase activity by 10-50% Homo sapiens
3.5.4.10 N2-acetyl-2'deoxyguanosine 5'-monophosphate decreased IMP cyclohydrolase activity by 10-50% Homo sapiens
3.5.4.10 N6-(carboxymethyl)adenosine 5'-monophosphate strong competitive inhibitor Homo sapiens
3.5.4.10 xanthosine 5'-monophosphate strong competitive inhibitor Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.1.2.3 64400
-
2 * 64400, deduced from nucleotide sequence of cDNA Homo sapiens
3.5.4.10 62100
-
2 * 62100, protein mobility assay Homo sapiens

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-imidazolecarboxamide Bacillus subtilis
-
tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide Escherichia coli
-
tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide Homo sapiens de novo synthesis of purine nucleotides tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide Gallus sp. de novo synthesis of purine nucleotides tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
3.5.4.10 5-formamido-1-(5-phosphoribosyl)imidazole-4-carboxamide Homo sapiens de novo purine synthesis step 10 ?
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.1.2.3 Bacillus subtilis
-
-
-
2.1.2.3 Escherichia coli
-
-
-
2.1.2.3 Gallus sp.
-
chicken
-
2.1.2.3 Gallus sp.
-
avian
-
2.1.2.3 Homo sapiens
-
human
-
3.5.4.10 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.1.2.3
-
Homo sapiens
3.5.4.10 780fold to apparent homogeneity Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.2.3 CCRF-CEM cell leukemia cell, T lymphoblastoid cell line Homo sapiens
-
2.1.2.3 liver
-
Homo sapiens
-
2.1.2.3 liver
-
Gallus sp.
-
2.1.2.3 MCF-7 cell breast cancer cell Homo sapiens
-
3.5.4.10 CEM cell
-
Homo sapiens
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.1.2.3 0.00067
-
-
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-imidazolecarboxamide
-
Bacillus subtilis tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide
-
Escherichia coli tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide de novo synthesis of purine nucleotides Homo sapiens tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
2.1.2.3 10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide de novo synthesis of purine nucleotides Gallus sp. tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
r
2.1.2.3 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 Bacillus subtilis ?
-
?
2.1.2.3 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 ?
-
?
2.1.2.3 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 ?
-
?
2.1.2.3 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 Gallus sp. ?
-
?
2.1.2.3 N10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide
-
Bacillus subtilis tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide
-
r
2.1.2.3 N10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide
-
Escherichia coli tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide
-
r
2.1.2.3 N10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide
-
Homo sapiens tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide
-
r
2.1.2.3 N10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide
-
Gallus sp. tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide
-
r
3.5.4.10 5-formamido-1-(5-phosphoribosyl)imidazole-4-carboxamide de novo purine synthesis step 10 Homo sapiens ?
-
?
3.5.4.10 5-formamidoimidazole-4-carboxamide
-
Homo sapiens hypoxanthine + H2O
-
ir

Subunits

EC Number Subunits Comment Organism
2.1.2.3 dimer
-
Gallus sp.
2.1.2.3 dimer 2 * 64400, deduced from nucleotide sequence of cDNA Homo sapiens
3.5.4.10 dimer 2 * 62100, protein mobility assay Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.1.2.3 5-aminoimidazole-4-carboxamide ribotide transformylase-IMP cyclohydrolase bifunctional enzyme Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.5.4.10 37
-
-
Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.5.4.10 7.4
-
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.5.4.10 0.0000011
-
IC50-value in cell culture 0.0011 microM Homo sapiens adenosine N1-oxide 5'-monophosphate
3.5.4.10 0.0002
-
IC50-value in cell culture 0.0002 mM Homo sapiens 2-fluoroadenine arabinoside 5'-monophosphate
3.5.4.10 0.0075
-
IC50-value in cell culture 0.0075 mM Homo sapiens 6-mercaptopurine riboside 5'-monophosphate