Literature summary for 2.1.2.3 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.

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Crystallization (Commentary)

Crystallization (Comment)	Organism
sitting drop vapor diffusion method, co-crystallized in the presence of substrate with BW1540 and BW2315	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
BW1540	sulfamido-bridged 5,8-dideazafolate analogue	Homo sapiens
BW2315	sulfamido-bridged 5,8-dideazafolate analogue	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-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
Homo sapiens	P31939	-	-

Substrates and Products (Substrate)

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

Subunits

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

Synonyms

Synonyms	Comment	Organism
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	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.000006	-	BW2315	-	Homo sapiens
0.000008	-	BW1540	-	Homo sapiens

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Release 2023.1 (January 2023)