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Literature summary for 4.2.99.18 extracted from

  • Srinivasan, A.; Wang, L.; Cline, C.J.; Xie, Z.; Sobol, R.W.; Xie, X.Q.; Gold, B.
    Identification and characterization of human apurinic/apyrimidinic endonuclease-1 inhibitors (2012), Biochemistry, 51, 6246-6259.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 4.2.99.18

Crystallization (Commentary)

Crystallization (Comment) Organism
molecular modeling of inhibitors to crystal structure, PDB entry 1DE8 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-methyl-4-[(1E)-1-[2-(6-methyl[1,3]dioxolo[4,5-g]quinolin-8-yl)hydrazinylidene]ethyl]-2-phenyl-1,2-dihydro-3H-pyrazol-3-one inhibitor induces time-dependent increases in the accumulation of abasic sites in cells at levels that correlate with its potency to inhibit APE-1 endonuclease excision. The inhibitor also potentiates by 5fold the toxicity of a DNA methylating agent that creates abasic sites Homo sapiens
8-[(2E)-2-(3-methoxybenzylidene)hydrazinyl]-6-methyl[1,3]dioxolo[4,5-g]quinoline inhibitor induces time-dependent increases in the accumulation of abasic sites in cells at levels that correlate with its potency to inhibit APE-1 endonuclease excision. The inhibitor also potentiates by 5fold the toxicity of a DNA methylating agent that creates abasic sites Homo sapiens
8-[(2E)-2-[(9-ethyl-9H-carbazol-3-yl)methylidene]hydrazinyl]-6-methyl[1,3]dioxolo[4,5-g]quinoline inhibitor induces time-dependent increases in the accumulation of abasic sites in cells at levels that correlate with its potency to inhibit APE-1 endonuclease excision. The inhibitor also potentiates by 5fold the toxicity of a DNA methylating agent that creates abasic sites Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P27695
-
-

Synonyms

Synonyms Comment Organism
APE-1
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00012
-
 8-[(2E)-2-[(9-ethyl-9H-carbazol-3-yl)methylidene]hydrazinyl]-6-methyl[1,3]dioxolo[4,5-g]quinoline pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.00018
-
 1-methyl-4-[(1E)-1-[2-(6-methyl[1,3]dioxolo[4,5-g]quinolin-8-yl)hydrazinylidene]ethyl]-2-phenyl-1,2-dihydro-3H-pyrazol-3-one pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.00019
-
 8-[(2E)-2-(3-methoxybenzylidene)hydrazinyl]-6-methyl[1,3]dioxolo[4,5-g]quinoline pH not specified in the publication, temperature not specified in the publication Homo sapiens