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Literature summary for 5.6.2.1 extracted from

  • Jun, K.Y.; Lee, E.Y.; Jung, M.J.; Lee, O.H.; Lee, E.S.; Park Choo, H.Y.; Na, Y.; Kwon, Y.
    Synthesis, biological evaluation, and molecular docking study of 3-(3-heteroatom substituted-2-hydroxy-1-propyloxy) xanthone analogues as novel topoisomerase IIalpha catalytic inhibitor (2011), Eur. J. Med. Chem., 46, 1964-1971.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-hydroxy-3-(oxiran-2-ylmethoxy)-9H-xanthen-9-one
-
Homo sapiens
1-hydroxy-3-[2-hydroxy-3-[(2-hydroxyethyl)amino]propoxy]-9H-xanthen-9-one 1.1% inhibition at 0.02 mM Homo sapiens
1-hydroxy-3-[2-hydroxy-3-[(3-hydroxypropyl)amino]propoxy]-9H-xanthen-9-one 3.5% inhibition at 0.02 mM Homo sapiens
camptothecin
-
Homo sapiens
etoposide
-
Homo sapiens
additional information molecular docking study, overview. No inhibition by 3-[3-[bis(2-hydroxyethyl)amino]-2-hydroxypropoxy]-1-hydroxy-9H-xanthen-9-one, 1-hydroxy-3-[2-hydroxy-3-[(3-hydroxypropyl)sulfanyl]propoxy]-9H-xanthen-9-one, 1-hydroxy-3-[2-hydroxy-3-[(2-hydroxyethyl)sulfanyl]propoxy]-9H-xanthen-9-one, 1-hydroxy-3-[2-hydroxy-3-(propylamino)propoxy]-9H-xanthen-9-one, 1-hydroxy-3-[2-hydroxy-3-(2-hydroxyethoxy)propoxy]-9H-xanthen-9-one, and 3-[3-[(2-chloroethyl)sulfanyl]-2-hydroxypropoxy]-1-hydroxy-9H-xanthen-9-one Homo sapiens
novobiocin inhibits the ATPase activity Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
Homo sapiens 5634
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
DU-145 cell
-
Homo sapiens
-
HCT-116 cell
-
Homo sapiens
-
HeLa cell
-
Homo sapiens
-
HL-60 cell
-
Homo sapiens
-
MDA-MB-231 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information substrate for DNA topo I is supercoiled pBR322 plasmid DNA Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
Topo I
-
Homo sapiens
Topoisomerase I
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.9
-
assay at Homo sapiens