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Literature summary for 2.1.2.3 extracted from

  • 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 (2009), Biochem. Pharmacol., 77, 1161-1172.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)-gamma-glutamyl-gamma-glutamyl-gamma-glutamyl-gamma-glutamylglutamic acid
-
Homo sapiens
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)-gamma-glutamyl-gamma-glutamylglutamic acid
-
Homo sapiens
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid
-
Homo sapiens
N-([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,3-dihydrothiophen-2-yl]carbonyl)-4-methylideneglutamic acid
-
Homo sapiens
N-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
Homo sapiens
N-[4-[2-(2,4-diaminopyrido[3,2-d]pyrimidin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
Homo sapiens
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2-fluorobenzoyl]-4-methylideneglutamic acid
-
Homo sapiens
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
Homo sapiens
N-[4-[2-(2-amino-4-methylquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
CCRF-CEM cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
10-formyl-tetrahydrofolic acid + 5'-phosphoribosyl-5-amino-imidazole-carboxamide
-
Homo sapiens 5,6,7,8-tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide
-
Homo sapiens tetrahdrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?

Synonyms

Synonyms Comment Organism
5-amino-4-imidazolecarboxamide ribotide formyltransferase
-
Homo sapiens
AICAR formyltransferase
-
Homo sapiens
AICARFT
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
value above 0.05 Homo sapiens N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid
additional information
-
value above 0.05 Homo sapiens N-[4-[2-(2-amino-4-methylquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
additional information
-
value above 0.05 Homo sapiens N-([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,3-dihydrothiophen-2-yl]carbonyl)-4-methylideneglutamic acid
additional information
-
value above 0.05 Homo sapiens N-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-4-methylideneglutamic acid
additional information
-
value above 0.05 Homo sapiens N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2-fluorobenzoyl]-4-methylideneglutamic acid
additional information
-
value above 0.05 Homo sapiens N-[4-[2-(2,4-diaminopyrido[3,2-d]pyrimidin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
additional information
-
value above 0.05 Homo sapiens N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid