Information on EC 2.1.2.3 - phosphoribosylaminoimidazolecarboxamide formyltransferase and Organism(s) Homo sapiens and UniProt Accession P31939

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658026

formyl group transfer

Biosynthesis of secondary metabolites, One carbon pool by folate, Purine metabolism

BRENDA

purine metabolism

KEGG

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-, -

10-formyltetrahydrofolate:5'-phosphoribosyl-5-amino-4-imidazole-carboxamide N-formyltransferase

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9032-03-5

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(6R,6S)-10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide

tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide

-

-

r

10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide

tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide

10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide

tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide

penultimate and final steps in the de novo purine biosynthesis pathway

-

r

10-formyltetrahydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide

tetrahydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide

-

736802, 757016, 757394

-

?

N10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide

tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide

-

-

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

10-formyl-tetrahydrofolic acid + 5'-phosphoribosyl-5-amino-imidazole-carboxamide

5,6,7,8-tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide

-

-

?

10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide

tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide

10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide

tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide

10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide

tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide

10-formyltetrahydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide

tetrahydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide

10-formyltetrahydrofolate + 5-amino-imidazole-4-thiocarboxamide ribonucleotide

tetrahydrofolate + 6-mercaptopurine ribonucleotide

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-

?

N10-formyltetrahydrofolic acid + 5-amino-4-imidazole carboxamide ribonucleotide

tetrahydrofolic acid + 5-formamido-4-imidazole carboxamide ribonucleotide

8 entries

additional information

?

-

13 entries

10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide

tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide

10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide

tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide

penultimate and final steps in the de novo purine biosynthesis pathway

-

r

10-formyltetrahydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide

tetrahydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide

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736802, 757016, 757394

-

?

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

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10-formyl-7,8-dihydrofolate is the in vivo substrate for AICAR transformylase

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r

10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide

tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide

-

penultimate step of the purine de novo synthesis pathway

658026

-

?

10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide

tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide

-

penultimate step of the purine de novo synthesis pathway

-

?

10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazolecarboxamide

tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazolecarboxamide

10-formyltetrahydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide

tetrahydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide

additional information

?

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3 entries

10-formyltetrahydrofolate

3 entries

10-formyldihydrofolate

-

10-formylfolate

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10-formyltetrahydrofolate

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658026, 658284, 673127

N10-formyl-7,8-dihydrofolate

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kinetically preferred over 10-formyl-5,6,7,8-tetrahydrofolate by AICAR transformylase

N10-formyltetrahydrofolate

-

485756, 485759, 485760

(S)-2-(5-(3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)propyl)thiophene-2-carboxamido)pentanedioic acid

inhibits de novo purine nucleotide rather than thymidylate biosynthesis via inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase

(S)-2-(5-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)butyl)thiophene-2-carboxamido)pentanedioic acid

inhibits de novo purine nucleotide rather than thymidylate biosynthesis via inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase

3-[(4-cyanobenzene-1-sulfonyl)amino]benzamide

-

4-amino-10-methylpteroylglutamic acid

methotrexate, non-competitive inhibitor

4-chloro-N-(1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl)benzene-1-sulfonamide

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4-cyano-N-(1-oxo-1,2-dihydroisoquinolin-7-yl)benzene-1-sulfonamide

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4-cyano-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)benzene-1-sulfonamide

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4-cyano-N-phenylbenzene-1-sulfonamide

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5-(5,5-dimethyl-6-oxo-1,4-dihydropyridin-3-yl)-N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)thiophene-2-sulfonamide

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5-(5-ethyl-5-methyl-6-oxo-1,4-dihydropyridin-3-yl)-N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)thiophene-2-sulfonamide

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5-[(3R,4S)-3-fluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide

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5-[(3S,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide

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5-[(4R)-3,3-difluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide

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5-[(4S)-3,3-difluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide

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BW1540

sulfamido-bridged 5,8-dideazafolate analogue

BW2315

sulfamido-bridged 5,8-dideazafolate analogue

calotropin

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dicrocin

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mauritine A

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melianone

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methotrexate

N-(2-amino-4-oxo-3,4-dihydroquinazolin-6-yl)-4-cyanobenzene-1-sulfonamide

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N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-(4-hydroxypiperidin-1-yl)thiophene-2-sulfonamide

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N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide

N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-(6-oxo-1H-pyridin-3-yl)thiophene-2-sulfonamide

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N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-[(3R)-3-hydroxy-1-piperidyl]thiophene-2-sulfonamide

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N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-[(3S)-3-hydroxy-1-piperidyl]thiophene-2-sulfonamide

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N-[(4-[[(2-amino-4-oxo-3,4-dihydroquinazolin-6-yl)amino]sulfonyl]-phenyl)carbonyl]-L-glutamic acid

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N-[(S)-(4-([(2-amino-4-hydroxy-quinazolin-6-yl)dihydroxy-lambda-4-sulfanyl]amino)phenyl)-hydroxymethyl]-L-glutamic acid

binding structure, docking study and crystal structure analysis

N-[4-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid

inhibits de novo purine nucleotide rather than thymidylate biosynthesis via inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase

N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid

inhibits de novo purine nucleotide rather than thymidylate biosynthesis via inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase

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

pemetrexed

uscharidin

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(6S/R)-5,10-dideaza-5,6,7,8,-tetrahydrofolate

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485758, 485759

(S)-2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)pentanedioic acid

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(S)-2-(4-(2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido)pentanedioic acid

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(S)-2-(4-(3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)propyl)benzamido)pentanedioic acid

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(S)-2-(4-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)butyl)benzamido)pentanedioic acid

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(S)-2-(4-(5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)pentyl)benzamido)pentanedioic acid

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(S)-2-(4-(6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)hexyl)benzamido)pentanedioic acid

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(S)-2-[2-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-acetylamino]-pentanedioic acid

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(S)-2-[2-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-ethylsulfanyl]-acetylamino]-pentanedioic acid

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(S)-2-[3-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-propionylamino]-pentanedioic acid

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(S)-2-[3-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-ethylsulfanyl]-propionylamino]-pentanedioic acid

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(S)-2-[4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-benzoylamino]-pentanedioic acid

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(S)-2-[4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-butyrylamino]-pentanedioic acid

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(S)-2-[5-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-pentanoylamino]-pentanedioic acid

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(S)-2-[6-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-hexanoylamino]-pentanedioic acid

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1-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetyl]-piperidine-4-carboxylic acid (pyridin-3-ylmethyl)-amide

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2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-N-[[(pyridin-3-ylmethyl)-carbamoyl]-methyl]-acetamide

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2-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-ethylsulfanyl]-N-pyridin-2-ylmethyl-acetamide

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2-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-ethylsulfanyl]-N-pyridin-3-ylmethyl-acetamide

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2-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-ethylsulfanyl]-N-pyridin-4-ylmethyl-acetamide

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2-[[([4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]phenyl]carbonyl)amino]methyl]-3-methylidenebutanedioic acid

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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

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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

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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

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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

3-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-propionamide

-

3-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-ethylsulfanyl]-N-pyridin-2-ylmethyl-propionamide

-

3-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-ethylsulfanyl]-N-pyridin-3-ylmethyl-propionamide

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3-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-ethylsulfanyl]-N-pyridin-4-ylmethyl-propionamide

-

4-([2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-methyl)-N-pyridin-3-ylmethyl-benzamide

-

inhibition of thymidylate synthase, as well as glycinamide ribonucleotide formyltransferase and ribonucleotide formyltransferase. Growth inhibition of 4-([2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-methyl)-N-pyridin-3-ylmethyl-benzamide toward KB cells results in cytotoxicity and G1/G2-phase accumulation, and is partially protected by excess thymidine and adenosine, but is completely reversed in the combination of thymidine and adenosine

4-8[2-(2-amino-4-oxo-4,4a,7,7a-tetrahydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)acetamido]methyl]-N-[(pyridin-3-yl)methyl]benzamide

-

4-amino-10-methylpteroylglutamic acid

-

methotrexate, non-competitive inhibitor

172161, 485754, 485758, 485760

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

-

4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-cyclohexanecarboxylic acid (pyridin-3-ylmethyl)-amide

-

4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-benzamide

-

4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-butyramide

-

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-formyl-5-aminoimidazole-4-carboxamide ribonucleotide

-

5-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-pentanoic acid (pyridin-3-ylmethyl)-amide

-

6-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-hexanoic acid (pyridin-3-ylmethyl)-amide

-

AMP

-

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

dihydrofolic acid pentaglutamate

-

KCl

-

lometrexol

-

methotrexate

-

N-(3-[[2-(2-amino-4-oxo-4,4a,7,7a-tetrahydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]sulfanyl]propanoyl)-L-glutamic acid

-

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-([[2-(2-amino-4-oxo-4,4a,7,7a-tetrahydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]sulfanyl]acetyl)-L-glutamic 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

-

pemetrexed

-

pralatrexate

-

sulphalazine

-

XMP

-

additional information

5 entries

-

additional information

enzyme phosphorylation by anaplastic lymphoma kinase enhances enzymatic activity and dampens the methotrexate-mediated transformylase activity inhibition

696946

-

0.0602

(6R,6S)-10-formyltetrahydrofolic acid

-

0.0168

5-aminoimidazole-4-carboxamide ribonucleotide

-

0.01

10-formyltetrahydrofolate

-

485759

0.01 - 0.019

5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide

0.0009

5-amino-imidazole-4-thiocarboxamide ribonucleotide

-

10-formyldihydrofolate as cofactor

0.0015 - 0.0168

5-aminoimidazole-4-carboxamide ribonucleotide

0.185

tetrahydrofolate

-

485759

additional information

-

10-formyl-7,8-dihydrofolate has an about 5fold kinetic advantage, Vm/Km, over 10-formyl-5,6,7,8-tetrahydrofolate for AICAR transformylases in human leukemia cells and for human recombinant AICAR transformylase

-

2.9 - 7

5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide

3 entries

0.000008

BW1540

-

0.000006

BW2315

-

0.000015

NSC30171

-

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

-

0.0007

5-amino-4-nitroimidazole ribonucleotide

-

0.0004

5-formyl-5-aminoimidazole-4-carboxamide ribonucleotide

-

0.027

AMP

-

0.003

Cappsin 1

-

0.0012

XMP

-

0.09

3-[(4-cyanobenzene-1-sulfonyl)amino]benzamide

Homo sapiens

at pH 7.5 and 25°C

0.0348

4-chloro-N-(1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl)benzene-1-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

0.000608

4-cyano-N-(1-oxo-1,2-dihydroisoquinolin-7-yl)benzene-1-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

0.000723

4-cyano-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)benzene-1-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

0.1

4-cyano-N-phenylbenzene-1-sulfonamide

Homo sapiens

IC50 above 0.1 mM, at pH 7.5 and 25°C

0.000005

5-(5,5-dimethyl-6-oxo-1,4-dihydropyridin-3-yl)-N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)thiophene-2-sulfonamide

Homo sapiens

IC50 below 0.000005 mM, at pH 7.5 and 25°C

0.000005

5-(5-ethyl-5-methyl-6-oxo-1,4-dihydropyridin-3-yl)-N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)thiophene-2-sulfonamide

Homo sapiens

IC50 below 0.000005 mM, at pH 7.5 and 25°C

0.00002

5-[(3R,4S)-3-fluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

0.0000078

5-[(3S,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

0.000012

5-[(4R)-3,3-difluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

0.000013

5-[(4S)-3,3-difluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

0.0181

N-(2-amino-4-oxo-3,4-dihydroquinazolin-6-yl)-4-cyanobenzene-1-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

0.000013

N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-(4-hydroxypiperidin-1-yl)thiophene-2-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

0.000014 - 0.000016

N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide

0.000005

N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-(6-oxo-1H-pyridin-3-yl)thiophene-2-sulfonamide

Homo sapiens

IC50 below 0.000005 mM, at pH 7.5 and 25°C

0.000026

N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-[(3R)-3-hydroxy-1-piperidyl]thiophene-2-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

0.000018

N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-[(3S)-3-hydroxy-1-piperidyl]thiophene-2-sulfonamide

Homo sapiens

at pH 7.5 and 25°C

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

nasopharyngeal carcinoma cell

additional information

N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid

1.19

-

0.00067

-

-

-

-

-

breast cancer cell

-

-

-

-

-

alveolar carcinoma cell

-

-

-

-

-

-

cervical carcinoma cell line

-

-

705032, 736059, 736610, 756643, 756648

-

-

172161, 485750, 485754

-

peripheral blood mononuclear cell

-

756643, 756648

-

-

-

the enzyme later accumulates in the Golgi/endosome network

the enzyme later accumulates in the Golgi/endosome network

-

AICAR transformylase does not form clusters

malfunction

metabolism

last and rate-limiting enzyme of the de novo purine synthesis pathway

736802

physiological function

metabolism

-

aminoimidazolecarboxamide ribotide transformylase is involved in the de novo purine nucleotide biosynthesis. No enzyme complex that generates 10-formyl-5,6,7,8-tetrahydrofolate and immediately channels or furnishes it to AICAR transformylase is needed because the first oxidation product of 10-formyl-5,6,7,8-tetrahydrofolate is 10-formyl-7,8-dihydrofolate that is utilized by this transformylase

physiological function

-

10-formyl-7,8-dihydrofolate, not 10-formyl-5,6,7,8-tetrahydrofolate, is the predominant in vivo substrate for mammalian aminoimidazolecarboxamide ribotide transformylase, an enzyme in purine nucleotide biosynthesis de novo, which introduces C2 into the purine ring

additional information

P31939 pBLAST

PUR9_HUMAN

592

0

64616

Swiss-Prot

Show Sequence

other Location (Reliability: 2)

64425

1 * 64425, calculated from amino acid sequence

64430

cDNA sequencing

64450

electrospray mass spectroscopy

65630

gel filtration

64400

-

2 * 64400, deduced from nucleotide sequence of cDNA

172161

65000

-

recombinant enzyme, SDS-PAGE

485754

dimer

crystal structure analysis, monomer contains two functionally independent domains transformylase and cyclohydrolase activities

monomer

1 * 64425, calculated from amino acid sequence

dimer

monomer

-

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

696946

crystal structure analysis of human enzyme complexed with the sulfamido-bridged N-[(S)-(4-([(2-amino-4-hydroxy-quinazolin-6-yl)dihydroxy-lambda-4-sulfanyl]amino)phenyl)-hydroxymethyl]-L-glutamic acid at 2.55 A resolution, PDB ID 1P4R

sitting drop vapor diffusion method, co-crystallized in the presence of substrate with BW1540 and BW2315

-

-

T116S

-

AICAR transformylase/inosine monophosphate cyclohydrolase 346C>G polymorphism

673127

additional information

-

several site directed mutants created with mutations in the inosine monophosphate cyclohydrolase domain of the enzyme

-

Ni-NTA agarose resin column chromatography and Superdex 200 gel filtration

recombinant protein using His-tag

-

-

172161, 485754, 485759, 702155, 756196

expressed in Escherichia coli BL21(DE3) cells

expressed in Escherichia coli BL21.DE3 as His-tag fusion protein

659419

gene ATIC, genotyping of single nucleotide polymorphisms

737222

purH gene, cloning and sequencing of cDNA, expressed in Escherichia coli

cloned from a hepatoma cDNA library

-

485758

cloned from a placenta cDNA library, overproduced in Escherichia coli

-

485754, 485758

expressed in Escherichia coli BL21(DE3) cells

-

756196

native and mutant proteins

-

diagnostics

enzyme variants are used to predict methotrexate response in juvenile idiopathic arthritis, overview

medicine

medicine

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

Biochemistry

33

14237-14245

1994

Bacillus subtilis, Escherichia coli, Gallus sp., Homo sapiens

7947835

Rayl, E.A.; Moroson, B.A.; Beardsley, G.P.

The human purH gene product, 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase. Cloning, sequencing, expression, purification, kinetic analysis, and domain mapping

J. Biol. Chem.

271

2225-2233

1996

Bacillus subtilis, Escherichia coli, Gallus sp., Homo sapiens (P31939), Homo sapiens, Salmonella enterica subsp. enterica serovar Typhimurium

8567683

485750

Ha, T.; Morgan, S.L.; Vaughn, W.H; Eto, I.; Baggott, J.E.

Detection of inhibition of 5-aminoimidazole-4-carboxamide ribotide transformylase by thioinosinic acid and azathioprine by a new colorimetric assay

Biochem. J.

272

339-342

1990

Gallus sp., Homo sapiens, Mus musculus

2268263

485754

Sugita, T.; Aya, H.; Ueno, M.; Ishizuka, T.; Kawashima, K.

Characterization of molecularly cloned human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase

J. Biochem.

122

309-313

1997

Bacillus subtilis, Homo sapiens, Salmonella enterica subsp. enterica serovar Typhimurium

9378707

Wall, M.; Shim, J.H.; Benkovic, S.J.

Human AICAR transformylase: Role of the 4-Carboxamide of AICAR in binding and catalysis

Biochemistry

39

11303-11311

2000

Escherichia coli, Homo sapiens

10985775

485757

Shim, J.H.; Wall, M.; Benkovic, S.J.; Diaz, N.; Suarez, D.; Merz, K.M., Jr.

Evaluation of the catalytic mechanism of AICAR transformylase by pH-dependent kinetics, mutagenesis, and quantum chemical calculations

J. Am. Chem. Soc.

123

4687-4696

2001

Bacillus subtilis, Escherichia coli, Gallus sp., Homo sapiens, Salmonella enterica subsp. enterica serovar Typhimurium

11457277

485758

Vergis, J.M.; Bulock, K.G.; Fleming, K.G.; Beardsley, G.P.

Human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase/inosine 5'-monophosphate cyclohydrolase. A bifunctional protein requiring dimerization for transformylase activity but not for cyclohydrolase activity

J. Biol. Chem.

276

7727-7733

2001

Gallus sp., Homo sapiens, Saccharomyces cerevisiae

11096114

485759

Bulock, K.G.; Beardsley, G.P.; Anderson, K.S.

The kinetic mechanism of the human bifunctional enzyme ATIC (5-amino-4-imidazolecarboxamide ribonucleotide transformylase/inosine 5'-monophosphate cyclohydrolase): A surprising lack of substrate channeling

J. Biol. Chem.

277

22168-22174

2002

Gallus sp., Homo sapiens

11948179

485760

Wolan, D.W.; Greasley, S.E.; Beardsley, G.P.; Wilson, I.A.

Structural insights into the avian AICAR transformylase mechanism

Biochemistry

41

15505-15513

2002

Gallus sp., Homo sapiens

12501179

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

J. Biol. Chem.

279

18034-18045

2004

Homo sapiens (P31939), Homo sapiens

14966129

658026

Vergis, J.M.; Beardsley, G.P.

Catalytic mechanism of the cyclohydrolase activity of human aminoimidazole carboxamide ribonucleotide formyltransferase/inosine monophosphate cyclohydrolase

Biochemistry

43

1184-1192

2004

aves, Homo sapiens

14756554

Capps, K.J.; Humiston, J.; Dominique, R.; Hwang, I.; Boger, D.L.

Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization

Bioorg. Med. Chem. Lett.

15

2840-2844

2005

Homo sapiens

15911265

659419

Xu, L.; Li, C.; Olson, A.J.; Wilson, I.A.

Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate inhibitor identified by virtual ligand screening

J. Biol. Chem.

279

50555-50565

2004

Gallus gallus (P31335), Homo sapiens (P31939)

15355974

Li, C.; Xu, L.; Wolan, D.W.; Wilson, I.A.; Olson, A.J.

Virtual screening of human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase against the NCI diversity set by use of AutoDock to identify novel nonfolate inhibitors

J. Med. Chem.

47

6681-6690

2004

Homo sapiens (P31939), Homo sapiens

15615517

673127

Gellekink, H.; Blom, H.J.; den Heijer, M.

Associations of common polymorphisms in the thymidylate synthase, reduced folate carrier and 5-aminoimidazole-4-carboxamide ribonucleotide transformylase/inosine monophosphate cyclohydrolase genes with folate and homocysteine levels and venous thrombosis

Clin. Chem. Lab. Med.

45

471-476

2007

Homo sapiens

17439323

696946

Boccalatte, F.E.; Voena, C.; Riganti, C.; Bosia, A.; DAmico, L.; Riera, L.; Cheng, M.; Ruggeri, B.; Jensen, O.N.; Goss, V.L.; Lee, K.; Nardone, J.; Rush, J.; Polakiewicz, R.D.; Comb, M.J.; Chiarle, R.; Inghirami, G.

The enzymatic activity of 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase is enhanced by NPM-ALK: new insights in ALK-mediated pathogenesis and the treatment of ALCL

Blood

113

2776-2790

2009

Homo sapiens (P31939)

18845790

McGuire, J.J.; Haile, W.H.

Metabolism-blocked antifolates as potential anti-rheumatoid arthritis agents: 4-amino-4-deoxy-5,8,10-trideazapteroyl-D,L-4-methyleneglutamic acid (CH-1504) and its analogs

Biochem. Pharmacol.

77

1161-1172

2009

Homo sapiens

19174154

Deng, Y.; Zhou, X.; Kugel Desmoulin, S.; Wu, J.; Cherian, C.; Hou, Z.; Matherly, L.H.; Gangjee, A.

Synthesis and biological activity of a novel series of 6-substituted thieno[2,3-d]pyrimidine antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors over the reduced folate carrier and proton-coupled folate transpo

J. Med. Chem.

52

2940-2951

2009

Homo sapiens

19371039

Baggott, J.E.; Tamura, T.

Evidence for the hypothesis that 10-formyldihydrofolate is the in vivo substrate for aminoimidazolecarboxamide ribotide transformylase

Exp. Biol. Med. (Maywood)

235

271-277

2010

Homo sapiens, Rattus norvegicus

20404044

Liu, Y.; Zhang, C.; Zhang, H.; Li, M.; Yuan, J.; Zhang, Y.; Zhou, J.; Guo, H.; Zhao, L.; Du, Y.; Wang, L.; Ren, L.

Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidines as potential nonclassical antifolates targeting both thymidylate and purine nucleotide biosynthesis

Eur. J. Med. Chem.

93

142-155

2015

Homo sapiens

25668494

Mitchell-Ryan, S.; Wang, Y.; Raghavan, S.; Ravindra, M.P.; Hales, E.; Orr, S.; Cherian, C.; Hou, Z.; Matherly, L.H.; Gangjee, A.

Discovery of 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as dual-acting inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis: Implications of inhibiting 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase to AMPK activation and anti-tumor activity

J. Med. Chem.

56

10016-10032

2013

Homo sapiens

24256410

Wang, Y.; Mitchell-Ryan, S.; Raghavan, S.; George, C.; Orr, S.; Hou, Z.; Matherly, L.H.; Gangjee, A.

Novel 5-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase and as potential antitumor agents

J. Med. Chem.

58

1479-1493

2015

Homo sapiens (P31939), Homo sapiens

25602637

736802

Boutchueng-Djidjou, M.; Collard-Simard, G.; Fortier, S.; Hebert, S.S.; Kelly, I.; Landry, C.R.; Faure, R.L.

The last enzyme of the de novo purine synthesis pathway 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase (ATIC) plays a central role in insulin signaling and the Golgi/endosomes protein network

Mol. Cell. Proteomics

14

1079-1092

2015

Homo sapiens (P31939), Rattus norvegicus (Q6IN16)

25687571

737222

Pastore, S.; Stocco, G.; Moressa, V.; Zandona, L.; Favretto, D.; Malusa, N.; Decorti, G.; Lepore, L.; Ventura, A.

5-Aminoimidazole-4-carboxamide ribonucleotide-transformylase and inosine-triphosphate-pyrophosphatase genes variants predict remission rate during methotrexate therapy in patients with juvenile idiopathic arthritis

Rheumatol. Int.

35

619-627

2015

Homo sapiens (P31939), Homo sapiens

25240429

756109

Witkowska, D.; Cox, H.L.; Hall, T.C.; Wildsmith, G.C.; Machin, D.C.; Webb, M.E.

Analysis of substrate binding in individual active sites of bifunctional human ATIC

Biochim. Biophys. Acta

1866

254-263

2018

Homo sapiens

29042184

756196

Davis, B.W.; Aumiller, W.M.; Hashemian, N.; An, S.; Armaou, A.; Keating, C.D.

Colocalization and sequential enzyme activity in aqueous biphasic systems experiments and modeling

Biophys. J.

109

2182-2194

2015

Homo sapiens

26588576

Liu, Y.; Li, M.; Zhang, H.; Yuan, J.; Zhang, C.; Zhang, K.; Guo, H.; Zhao, L.; Du, Y.; Wang, L.; Ren, L.

Design, synthesis and biological evaluation of 6-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of TS and AICARFTase and as potential antitumor agents

Eur. J. Med. Chem.

115

245-256

2016

Homo sapiens

27017552

Xing, R.; Zhang, H.; Yuan, J.; Zhang, K.; Li, L.; Guo, H.; Zhao, L.; Zhang, C.; Li, S.; Gao, T.; Liu, Y.; Wang, L.

Novel 6-substituted benzoyl and non-benzoyl straight chain pyrrolo[2,3-d]pyrimidines as potential antitumor agents with multitargeted inhibition of TS, GARFTase and AICARFTase

Eur. J. Med. Chem.

139

531-541

2017

Homo sapiens

28830032

757016

Markandeyan, D.; Kannaiyan, S.; Suresh, S.; Nimmakayala, R.; Ilamurugan, R.; Santhalingam, K.; Paul, B.

Virtual screening of phytochemicals for methotrexate like dihydrofolate reductase and aminoimidazole-4-carboxamide ribonucleotide (AICAR) transformylase inhibitory property using Molegro virtual docker

Int. J. Pharm. Pharm. Sci.

8

83-87

2016

Homo sapiens (P31939)

-