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Literature summary extracted from

  • Cheong, C.G.; Wolan, D.W.; Greasley, S.E.; Horton, P.A.; Beardsley, G.P.; Wilson, I.A.
    Crystal structures of human bifunctional enzyme aminoimidazole-4-carboxamide ribonucleotide transformylase/IMP cyclohydrolase in complex with potent sulfonyl-containing antifolates (2004), J. Biol. Chem., 279, 18034-18045.
    View publication on PubMed

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.1.2.3 sitting drop vapor diffusion method, co-crystallized in the presence of substrate with BW1540 and BW2315 Homo sapiens
3.5.4.10 in complex with transformylase inhibitors BW1540 and BW2315 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.2.3 BW1540 sulfamido-bridged 5,8-dideazafolate analogue Homo sapiens
2.1.2.3 BW2315 sulfamido-bridged 5,8-dideazafolate analogue 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-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 Homo sapiens P31939
-
-
3.5.4.10 Homo sapiens P31939 bifunctional enzyme aminoimidazole-4-carboxamide ribonucleotide transformylase/IMP cyclohydrolase
-

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
-
 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 Homo sapiens tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
 ?

Subunits

EC Number Subunits Comment Organism
2.1.2.3 dimer crystal structure analysis, monomer contains two functionally independent domains transformylase and cyclohydrolase activities Homo sapiens

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 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
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 0.000006
-
 BW2315
-
 Homo sapiens
2.1.2.3 0.000008
-
 BW1540
-
 Homo sapiens