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Literature summary for 2.5.1.49 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
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Inhibitors

Inhibitors Comment Organism Structure
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
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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HL-60 cell
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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