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Literature summary extracted from

  • Tang, C.; Zhang, Z.; Xu, B.; Li, M.; Liu, J.; Cui, J.
    Two newly synthesized 5-methyltetrahydrofolate-like compounds inhibit methionine synthase activity accompanied by cell cycle arrest in G1/S phase and apoptosis in vitro (2008), Anticancer Drugs, 19, 697-704.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.13 ZL-031 i.e. diethyl N-[4-[(2-[2,4-diamino-5-(2,3-dibromopropane)-5,6,7,8-tetrahydropyrido(3,2-d)pyrimidin-6-yl]methyl)amino]3-bromo-benzoyl]L-glutamate Homo sapiens
2.1.1.13 ZL-033 i.e. N-[4-[(2-[2,4-diamino-5-(2,3-dibromopropane)-5,6,7,8-tetrahydropyrido(3,2-d)pyrimidin-6-yl]methyl)amino]3-bromo-benzoyl]L-glutamic acid Homo sapiens
2.5.1.49 diethyl N-[[3-bromo-4-([[2,4-diamino-5-(2,3-dibromopropyl)-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl]methyl]amino)phenyl]carbonyl]glutamate inhibition of methionine synthase, arrest of cell cycle in G1/S phase and apoptosis. Treatment results in increase in cyclin E and cyclin-dependent kinase 2, reduction of caspase-3, poly(ADP-ribose) polymerase, caspase-8, and caspase-9 protein levels Homo sapiens
2.5.1.49 N-[[3-bromo-4-([[2,4-diamino-5-(2,3-dibromopropyl)-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl]methyl]amino)phenyl]carbonyl]glutamic acid inhibition of methionine synthase, arrest of cell cycle in G1/S phase and apoptosis. Treatment results in increase in cyclin E and cyclin-dependent kinase 2, reduction of caspase-3, poly(ADP-ribose) polymerase, caspase-8, and caspase-9 protein levels Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.13 Homo sapiens
-
-
-
2.5.1.49 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.13 HL-60 cell
-
Homo sapiens
-
2.5.1.49 HL-60 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.13 N5-methyltetrahydropteroylmonoglutamate + L-homocysteine
-
Homo sapiens tetrahydropteroylmonoglutamate + L-methionine
-
?

Synonyms

EC Number Synonyms Comment Organism
2.1.1.13 5-methyltetrahydrofolate-homocysteine methyltransferase
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.1.1.13 0.0014
-
at 37°C Homo sapiens ZL-033
2.1.1.13 0.01
-
at 37°C Homo sapiens ZL-031
2.5.1.49 0.0014
-
pH 7.2, 37°C Homo sapiens N-[[3-bromo-4-([[2,4-diamino-5-(2,3-dibromopropyl)-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl]methyl]amino)phenyl]carbonyl]glutamic acid
2.5.1.49 0.01
-
pH 7.2, 37°C Homo sapiens diethyl N-[[3-bromo-4-([[2,4-diamino-5-(2,3-dibromopropyl)-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl]methyl]amino)phenyl]carbonyl]glutamate