Information on EC 2.1.2.3 - phosphoribosylaminoimidazolecarboxamide formyltransferase

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria

EC NUMBER
COMMENTARY hide
2.1.2.3
-
RECOMMENDED NAME
GeneOntology No.
phosphoribosylaminoimidazolecarboxamide formyltransferase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
10-formyltetrahydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide = tetrahydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
formyl group transfer
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
Biosynthesis of antibiotics
-
-
Biosynthesis of secondary metabolites
-
-
inosine-5'-phosphate biosynthesis I
-
-
inosine-5'-phosphate biosynthesis II
-
-
Metabolic pathways
-
-
One carbon pool by folate
-
-
purine metabolism
-
-
Purine metabolism
-
-
SYSTEMATIC NAME
IUBMB Comments
10-formyltetrahydrofolate:5'-phosphoribosyl-5-amino-4-imidazole-carboxamide N-formyltransferase
-
CAS REGISTRY NUMBER
COMMENTARY hide
9032-03-5
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
onion
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
pigeon
-
-
Manually annotated by BRENDA team
carrot
-
-
Manually annotated by BRENDA team
-
UniProt
Manually annotated by BRENDA team
gene Rv0957
-
-
Manually annotated by BRENDA team
gene Rv0957
-
-
Manually annotated by BRENDA team
parsley
-
-
Manually annotated by BRENDA team
pea, L. var. Alaska
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
yeast
-
-
Manually annotated by BRENDA team
spinach
-
-
Manually annotated by BRENDA team
Trifolium sp.
trefoil
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(6R,6S)-10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide
tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide
show the reaction diagram
-
-
r
10-formyl-7,8-dihydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide
dihydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide
show the reaction diagram
10-formyl-7,8-dihydropteroylpenta-gamma-glutamate + 5'-phosphoribosyl-5-amino-4-imidazolecarboxamide
7,8-dihydropteroylpenta-gamma-glutarate + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
show the reaction diagram
-
-
-
?
10-formyl-8-deazafolate + 5'-phosphoribosyl-5-amino-4-imidazolecarboxamide
8-deazafolate + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
show the reaction diagram
-
-
-
?
10-formyl-tetrahydrofolic acid + 5'-phosphoribosyl-5-amino-imidazole-carboxamide
5,6,7,8-tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
show the reaction diagram
-
-
-
-
?
10-formyldihydrofolic acid pentaglutamate + 5'-phosphoribosyl-5-amino-4-imidazolecarboxamide
dihydrofolic acid pentaglutamate + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
show the reaction diagram
-
-
-
?
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide
tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
show the reaction diagram
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide
tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
show the reaction diagram
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide
tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
show the reaction diagram
10-formyltetrahydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide
tetrahydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide
show the reaction diagram
10-formyltetrahydrofolate + 5-amino-imidazole-4-thiocarboxamide ribonucleotide
tetrahydrofolate + 6-mercaptopurine ribonucleotide
show the reaction diagram
-
-
-
?
N10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide
tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide
show the reaction diagram
N10-formyltetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
tetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide
show the reaction diagram
-
-
-
-
?
N10-formyltetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
tetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
show the reaction diagram
-
-
-
?
N10-formyltetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamino-4-imidazole carboxamide ribonucleotide
tetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
show the reaction diagram
-
-
-
?
N10-formyltetrahydropteroylheptaglutamate + 5'-phosphoribosyl-5-formamino-4-imidazole carboxamide ribonucleotide
tetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
show the reaction diagram
-
-
-
?
N10-formyltetrahydropteroylhexaglutamate + 5'-phosphoribosyl-5-formamino-4-imidazole carboxamide ribonucleotide
tetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
show the reaction diagram
-
-
-
?
N10-formyltetrahydropteroylmonoglutamate + 5'-phosphoribosyl-5-formamino-4-imidazole carboxamide ribonucleotide
tetrahydropteroylmonoglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
show the reaction diagram
-
-
-
?
N10-formyltetrahydropteroylpentaglutamate + 5'-phosphoribosyl-5-formamino-4-imidazole carboxamide ribonucleotide
tetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
show the reaction diagram
-
-
-
?
N10-formyltetrahydropteroyltetraglutamate + 5'-phosphoribosyl-5-formamino-4-imidazole carboxamide ribonucleotide
tetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
show the reaction diagram
-
-
-
?
N10-formyltetrahydropteroyltriglutamate + 5'-phosphoribosyl-5-formamino-4-imidazole carboxamide ribonucleotide
tetrahydorpteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
show the reaction diagram
-
-
-
?
N5,N10-anhydroformyltetrahydrofolic acid + glycinamide ribonucleotide
N10-formyltetrahydrofolic acid + formylglycinamide ribonucleotide
show the reaction diagram
-
-
-
r
tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide
N10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide
show the reaction diagram
-
-
-
r
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
10-formyl-7,8-dihydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide
dihydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide
show the reaction diagram
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide
tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
show the reaction diagram
-
penultimate step of the purine de novo synthesis pathway
-
-
?
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide
tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
show the reaction diagram
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide
tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
show the reaction diagram
10-formyltetrahydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide
tetrahydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide
show the reaction diagram
N10-formyltetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide ribonucleotide
tetrahydropteroylglutamate + 5'-phosphoribosyl-5-formamido-4-imidazole carboxamide
show the reaction diagram
-
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
10-formyldihydrofolate
-
-
10-formylfolate
-
-
10-formyltetrahydrofolate
N10-formyl-7,8-dihydrofolate
N10-formyltetrahydrofolate
additional information
-
contains selenomethionine
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2RS)-N-[4-{1-(acetamideoxy)-3-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl)prop-2-yl}benzoyl]-L-glutamic acid
-
-
(2RS)-N-[4-{1-(acetoxy)-3-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl)prop-2-yl}benzoyl]-L-glutamic acid
-
-
(2RS)-N-[4-{3-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl)-1,1-(dimethoxy)prop-2-yl}benzoyl]-L-glutamic acid
-
-
(2RS)-N-[4-{3-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl)-1-(1,1-bromoacetoxy)prop-2-yl}benzoyl]-L-glutamic acid
-
-
(2RS)-N-[4-{3-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl)-1-(1,1-dimethoxyacetoxy)prop-2-yl}benzoyl]-L-glutamic acid
-
-
(2RS)-N-[4-{3-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl)-1-(ethoxalyoxy) prop-2-yl}benzoyl]-L-glutamic acid
-
-
(2RS)-N-[4-{3-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl)-1-(formyloxy)prop-2-yl}benzoyl]-L-glutamic acid
-
-
(2RS)-N-[4-{3-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl)-1-(hydroxy)prop-2-yl}benzoyl]-L-glutamic acid
-
-
(2RS)-N-[4-{3-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl)-1-(pyruvoyloxy)prop-2-yl}benzoyl]-L-glutamic acid
-
-
(6S/R)-5,10-dideaza-5,6,7,8,-tetrahydrofolate
-
-
10-formyl-5,6,7,8-tetrahydropteroylpenta-gamma-glutamate
-
-
10-formyl-5,8,10-trideazafolate
-
-
10-formylfolic acid pentaglutamate
-
competitive inhibitor
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
2-[[([4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]phenyl]carbonyl)amino]methyl]-3-methylidenebutanedioic acid
-
weak inhibition of enzymes of folate metabolism relevant to rheumatoid arthritis therapy such as thymidylate synthase EC 2.1.1.45, two formyltransferases of purine biosynthesis EC 2.1.2.2 and EC 2.1.2.3, and 5,10-methylenetetrahydrofolate reductase EC 1.5.1.20. Potent inhibition of dihydrofolate reductase
2-[[([4-[2-(2,4-diaminopyrido[3,2-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)amino]methyl]-3-methylidenebutanedioic acid
-
weak inhibition of enzymes of folate metabolism relevant to rheumatoid arthritis therapy such as thymidylate synthase EC 2.1.1.45, two formyltransferases of purine biosynthesis EC 2.1.2.2 and EC 2.1.2.3, and 5,10-methylenetetrahydrofolate reductase EC 1.5.1.20. Potent inhibition of dihydrofolate reductase
2-[[([4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2-fluorophenyl]carbonyl)amino]methyl]-3-methylidenebutanedioic acid
-
weak inhibition of enzymes of folate metabolism relevant to rheumatoid arthritis therapy such as thymidylate synthase EC 2.1.1.45, two formyltransferases of purine biosynthesis EC 2.1.2.2 and EC 2.1.2.3, and 5,10-methylenetetrahydrofolate reductase EC 1.5.1.20. Potent inhibition of dihydrofolate reductase
2-[[([4-[2-(2-amino-4-methylquinazolin-6-yl)ethyl]phenyl]carbonyl)amino]methyl]-3-methylidenebutanedioic acid
-
weak inhibition of enzymes of folate metabolism relevant to rheumatoid arthritis therapy such as thymidylate synthase EC 2.1.1.45, two formyltransferases of purine biosynthesis EC 2.1.2.2 and EC 2.1.2.3, and 5,10-methylenetetrahydrofolate reductase EC 1.5.1.20. Potent inhibition of dihydrofolate reductase
-
2-[[([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,5-dihydrothiophen-2-yl]carbonyl)amino]methyl]-3-methylidenebutanedioic acid
-
weak inhibition of enzymes of folate metabolism relevant to rheumatoid arthritis therapy such as thymidylate synthase EC 2.1.1.45, two formyltransferases of purine biosynthesis EC 2.1.2.2 and EC 2.1.2.3, and 5,10-methylenetetrahydrofolate reductase EC 1.5.1.20. Potent inhibition of dihydrofolate reductase
4-acetamidophenol
-
-
4-amino-10-methylpteroyl-gamma-glutamyl-gamma-glutamyl-gamma-glutamylglutamic acid
-
methotrexate polyglutamate, competitive inhibitor
4-amino-10-methylpteroylglutamic acid
4-amino-4-deoxy-5,8,10-trideazapteroyl-D,L-40-methyleneglutamic acid
-
weak inhibition of enzymes of folate metabolism relevant to rheumatoid arthritis therapy such as thymidylate synthase EC 2.1.1.45, two formyltransferases of purine biosynthesis EC 2.1.2.2 and EC 2.1.2.3, and 5,10-methylenetetrahydrofolate reductase EC 1.5.1.20. Potent inhibition of dihydrofolate reductase
4-N-allyl-5-aminoimidazole-4-carboxamide ribonucleotide
-
-
4-N-methyl-5-aminoimidazole-4-carboxamide ribonucleotide
-
-
5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide
-
product inhibitor
5-amino-1-beta-D-ribofuranosylimidazole 5'-phosphate
-
-
5-amino-1-beta-D-ribofuranosylimidazole-4-carbonitrile 5'-phosphate
-
-
5-amino-1-beta-D-ribofuranosylimidazole-4-carboxamidoxime 5'-phosphate
-
-
5-amino-1-beta-D-ribofuranosylimidazole-4-carboxylate 5'-phosphate
-
-
5-amino-4-nitro-1-beta-D-ribofuranosylimidazole 5'-phosphate
-
-
5-amino-4-nitroimidazole ribonucleotide
-
-
5-formyl-5-aminoimidazole-4-carboxamide ribonucleotide
7,8-dihydropteroylpenta-gamma-glutamate
-
-
Acid Yellow 17
-
IC50: 0.012 mM
Azathioprine
beta-DADF
-
IC50 125 nM
BW1540
-
sulfamido-bridged 5,8-dideazafolate analogue
BW2315
-
sulfamido-bridged 5,8-dideazafolate analogue
Cappsin 1
-
non-competitive, inhibition of activity by preventing the formation of dimers
-
Cappsin 2
-
some derivatives of Cappepsin are also inhibitory, inhibition of activity by preventing the formation of dimers
-
Cu2+
-
-
dihydrofolic acid pentaglutamate
folic acid pentaglutamate
-
competitive inhibitor
Ibuprofen
methotrexate
N-(4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-propyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-butyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[5-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-pentyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[6-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-hexyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)-gamma-glutamyl-gamma-glutamyl-gamma-glutamyl-gamma-glutamylglutamic acid
-
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)-gamma-glutamyl-gamma-glutamylglutamic acid
-
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid
-
-
N-([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,3-dihydrothiophen-2-yl]carbonyl)-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminopyrido[3,2-d]pyrimidin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2-fluorobenzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2-amino-4-methylquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N10-formyltetrahydropteroylglutamate
-
-
naproxen
NCI324571-C
-
IC50: 0.042 mM
NCI324572-F
-
IC50: 0.012 mM
NCI3262203-A
-
IC50: 0.012 mM
NCI47729-M
-
IC50: 0.003 mM
NSC126445
-
IC50: 0.010mM
NSC170645
-
IC50: 0.036 mM
NSC26699
-
IC50: 0.017 mM
NSC292213
-
IC50: 0.009 mM
NSC30171
-
IC50: 0.0006 mM
NSC321237
-
IC50: 0.106 mM
NSC324571
-
IC50: 0.020 mM
NSC324572
-
IC50: 0.012 mM
NSC324981
-
IC50: 0.020 mM
NSC326203
-
IC50: 0.012 mM
NSC326211
-
IC50: 0.204 mM
NSC37031
-
IC50: 0.008 mM
NSC37173
-
IC50: 0.004 mM
NSC41806
-
IC50: 0.055 mM
NSC45592
-
IC50: 0.012 mM
NSC47729
-
IC50: 0.003 mM
NSC58046
-
IC50: 0.008 mM
NSC7524
-
IC50: 0.231 mM
NSC88915
-
IC50: 0.014 mM
paracetamol
-
-
pteroylpenta-gamma-glutamate
-
-
SALOR2
-
IC50: 0.0014 mM
sulphalazine
-
-
thioinosinic acid
tylenol
-
-
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
enzyme phosphorylation by anaplastic lymphoma kinase enhances enzymatic activity and dampens the methotrexate-mediated transformylase activity inhibition
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0602
(6R,6S)-10-formyltetrahydrofolic acid
-
0.00051
10-formyldihydrofolic acid pentaglutamate
-
-
0.0043 - 0.2
10-formyltetrahydrofolate
0.031
5'-phosphoribosyl-5-amino-imidazolecarboxamide
-
-
0.0009
5-amino-imidazole-4-thiocarboxamide ribonucleotide
-
10-formyldihydrofolate as cofactor
0.0005 - 0.0168
5-aminoimidazole-4-carboxamide ribonucleotide
0.00183 - 0.00313
N10-formyltetrahydropteroylheptaglutamate
0.00164 - 0.00195
N10-formyltetrahydropteroylhexaglutamate
0.00165 - 0.353
N10-formyltetrahydropteroylmonoglutamate
0.00206 - 0.00256
N10-formyltetrahydropteroylpentaglutamate
0.00099 - 0.00107
N10-formyltetrahydropteroyltetraglutamate
0.00595 - 0.674
N10-formyltetrahydropteroyltriglutamate
0.185
tetrahydrofolate
-
-
0.00023
tetrahydrofolic acid
-
-
additional information
additional information
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00137
10-formylfolic acid pentaglutamate
-
-
0.007
2-[5-hydroxy-3-methyl-1-(2-methyl-4-sulfophenyl)-1H-pyrazo]-4-sulfobenzoic acid
-
pH 7.5
0.006
5-amino-1-beta-D-ribofuranosylimidazole 5'-phosphate
-
-
0.026
5-amino-1-beta-D-ribofuranosylimidazole-4-carbonitrile 5'-phosphate
-
-
0.01
5-amino-1-beta-D-ribofuranosylimidazole-4-carboxylate 5'-phosphate
-
-
0.0007
5-amino-4-nitro-1-beta-D-ribofuranosylimidazole 5'-phosphate
-
-
0.00004 - 0.0007
5-amino-4-nitroimidazole ribonucleotide
0.00007 - 0.0004
5-formyl-5-aminoimidazole-4-carboxamide ribonucleotide
0.027
AMP
-
-
0.09 - 0.12
Azathioprine
0.000008
BW1540
-
-
0.000006
BW2315
-
-
0.003
Cappsin 1
-
-
-
0.00014
dihydrofolic acid pentaglutamate
-
-
0.00008
folic acid pentaglutamate
-
-
0.075
methotrexate
-
-
0.00315
methotrexate polyglutamate
-
-
0.000015
NSC30171
-
-
0.039 - 0.11
thioinosinic acid
0.0012
XMP
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.012
2-[5-hydroxy-3-methyl-1-(2-methyl-4-sulfophenyl)-1H-pyrazo]-4-sulfobenzoic acid
0.000125
beta-DADF
Gallus gallus
-
IC50 125 nM
0.042
NCI324571-C
Gallus gallus
-
IC50: 0.042 mM
0.012
NCI324572-F
0.003
NCI47729-M
Gallus gallus
-
IC50: 0.003 mM
0.01
NSC126445
Homo sapiens
-
IC50: 0.010mM
0.036
NSC170645
Homo sapiens
-
IC50: 0.036 mM
0.017
NSC26699
Homo sapiens
-
IC50: 0.017 mM
0.009
NSC292213
Homo sapiens
-
IC50: 0.009 mM
0.0006
NSC30171
Homo sapiens
-
IC50: 0.0006 mM
0.106
NSC321237
Homo sapiens
-
IC50: 0.106 mM
0.02
NSC324571
Homo sapiens
-
IC50: 0.020 mM
0.012
NSC324572
Homo sapiens
-
IC50: 0.012 mM
0.02
NSC324981
Homo sapiens
-
IC50: 0.020 mM
0.012
NSC326203
Homo sapiens
-
IC50: 0.012 mM
0.204
NSC326211
Homo sapiens
-
IC50: 0.204 mM
0.008
NSC37031
Homo sapiens
-
IC50: 0.008 mM
0.004
NSC37173
Homo sapiens
-
IC50: 0.004 mM
0.055
NSC41806
Homo sapiens
-
IC50: 0.055 mM
0.012
NSC45592
Homo sapiens
-
IC50: 0.012 mM
0.003
NSC47729
Homo sapiens
-
IC50: 0.003 mM
0.008
NSC58046
Homo sapiens
-
IC50: 0.008 mM
0.231
NSC7524
Homo sapiens
-
IC50: 0.231 mM
0.014
NSC88915
Homo sapiens
-
IC50: 0.014 mM
0.0014
SALOR2
Gallus gallus
-
IC50: 0.0014 mM
additional information
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.00067
-
-
0.0371
-
-
0.856
-
-
additional information
-
1 unit = removal of 0.0001 mM of AICA-ribotide/0.5 ml/20 min at 37°C
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6 - 10.5
-
-
6.5 - 8.5
-
-
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0 - 50
-
-
pI VALUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5.49
-
calculated isoelectric point
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
-
Manually annotated by BRENDA team
-
cervical carcinoma cell line
Manually annotated by BRENDA team
-
hepatocellular carcinoma cell line
Manually annotated by BRENDA team
-
breast cancer cell
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
AICAR transformylase does not form clusters
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
49700
-
monomer, residues 1-452
64430
cDNA sequencing
64450
electrospray mass spectroscopy
65000
-
recombinant enzyme, SDS-PAGE
65630
gel filtration
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
bifunctional 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase associates with nucleoplasmin-anaplastic lymphoma kinase, and its phosphorylation requires anaplastic lymphoma kinase activity. Phosphorylation enhances enzymatic activity and dampens the methotrexate-mediated transformylase activity inhibition
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
purified recombinant His6-tagged PurH, without methylation of the 28 lysine residues, sitting drop vapour diffusion method, mixing of 0.001 ml of 56 mg/ml protein in 0.8 M sodium/potassium hydrogen phosphate, pH 7.5, with 0.001 ml of reservoir solution containing 0.1 M sodium acetate, pH 5.0, 1 M ammonium sulfate, 1 week to 1 month, X-ray diffraction structure determination and analysis at 3.05 A resolution
-
crystallized in complex with its inhibitor 2-[5-hydroxy-3-methyl-1-(2-methyl-4-sulfophenyl)-1H-pyrazo]-4-sulfobenzoic acid
-
recombinant His-tag fusion protein crystallized by sitting drop vapor diffusion method in complex with its inhibitor beta-DADF
-
ATIC complex crystallized in monoclinic space group P2(1), a = 56.48 A, b = 107.88 A, c = 103.86 A and beta = 91.2°
-
ATIC complex crystallized in monoclinic space group P2(1), a = 56.48 A, b = 107.88 A, c = 103.86 A and beta = 91.2°; crystallized in a binary complex with methotrexate, single crystal at 96 K to 2.3 A resolution, monoclinic crystals, space group P2(1), with unit-cell dimensions a = 65.17, B = 105.93, c= 103.47 A, beta = 108.27 degrees
-
sitting drop vapor diffusion method, co-crystallized in the presence of substrate with BW1540 and BW2315
-
purified recombinant His-tagged enzyme free or in complex with substrate 5-aminoimidazole-4-carboxamide ribonucleotide, both with adventitiously active site-bound nucleotide inhibitor of the cyclohydrolase activity, X-ray diffraction structure determination and analysis at 2.5 A and 2.2 A resolution, respectively
-
the three-dimensional structure of TM1249 is determined to 1.88 A resolution by molecular replacement
-
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
much less stable during storage in maleate buffer than in Tris or phosphate solutions
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
2°C, if the solution of purified enzyme are stored for 3 or 4 months, a requirement for a specific formyl donor can then be shown
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
inosinicase activity copurifies
-
partially
-
recombinant avian ATIC, purified from E. coli expression system
-
recombinant N-terminally His6-tagged MtbATIC in Escherichia coli strain BL21(DE3) by nickel affinity chromatography
-
recombinant N-terminally His6-tagged PurH from Escherichia coli strain Rosetta (DE3) by nickel affinity chromatography and gel filtration
-
recombinant protein using His-tag
using a nickel-chelating resin and a Resource Q column
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
ATICcDNA cloned into a pET28a vector and transformed into Escherichia coli BL21.DE3 for overexpression
-
cloned and expressed
cloned from a hepatoma cDNA library; cloned from a placenta cDNA library, overproduced in Escherichia coli
-
cloned from a placenta cDNA library, overproduced in Escherichia coli
-
expressed in Escherichia coli as His-tag fusion protein
-
expressed in Escherichia coli BL21.DE3 as His-tag fusion protein
expression of N-terminally His6-tagged MtbATIC in Escherichia coli strain BL21(DE3)
-
gene purH, expression of N-terminally His6-tagged PurH in Escherichia coli strain Rosetta (DE3)
-
into the plasmid pMH4 for expression in the Escherichia coli strain GeneHogs
-
native and mutant proteins
-
purH gene cloning and sequencing of cDNA
-
purH gene, cloning and sequencing of cDNA, expressed in Escherichia coli
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
T116S
-
AICAR transformylase/inosine monophosphate cyclohydrolase 346C>G polymorphism
additional information
-
several site directed mutants created with mutations in the inosine monophosphate cyclohydrolase domain of the enzyme
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
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