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Literature summary for 5.6.2.1 extracted from

  • Galvez-Peralta, M.; Hackbarth, J.S.; Flatten, K.S.; Kaufmann, S.H.; Hiasa, H.; Xing, C.; Ferguson, D.M.
    On the role of topoisomerase I in mediating the cytotoxicity of 9-aminoacridine-based anticancer agents (2009), Bioorg. Med. Chem. Lett., 19, 4459-4462.
    View publication on PubMedView publication on EuropePMC

Protein Variants

Protein Variants Comment Organism
additional information enzyme downregulation by topoisomerase I siRNA in HeLa cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(9-([2-(1H-Indol-3-yl)ethyl]amino)-3-acridinyl)(4-methyl-1-piperazinyl)methanone
-
Homo sapiens
(9-([2-(1H-indol-3-yl)ethyl]amino)acridin-3-yl)(4-methylpiperazin-1-yl)methanone
-
Homo sapiens
(9-([2-(1H-indol-3-yl)ethyl]amino)acridin-4-yl)(4-methylpiperazin-1-yl)methanone
-
Homo sapiens
(9-[(1-benzylpiperidin-4-yl)amino]acridin-3-yl)(4-methylpiperazin-1-yl)methanone
-
Homo sapiens
actinomycin D traps topoisomerase I-DNA covalent complexes Homo sapiens
amsacrine
-
Homo sapiens
camptothecin
-
Homo sapiens
doxorubicin inhibits the enzyme without trapping cleavable complexes Homo sapiens
additional information cytotoxicity and mechanism of action of a series of substituted 9-aminoacridines is evaluated using topoisomerase I and cancer cell growth inhibition assays, overview Homo sapiens
morpholinodoxorubicin traps topoisomerase I-DNA covalent complexes Homo sapiens
N,N-diethyl-9-([2-(1H-indol-3-yl)ethyl]amino)acridine-3-carboxamide
-
Homo sapiens
pyrazoloacridine completely suppresses the ability of topoisomerase I to relax supercoiled DNA at a concentration of 0.008 mM, inhibits the enzyme without trapping cleavable complexes 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
carcinoma cell
-
Homo sapiens
-
DU-145 cell
-
Homo sapiens
-
HCT-116 cell
-
Homo sapiens
-
MCF-7 cell
-
Homo sapiens
-
MEL cell melanoma cells Homo sapiens
-
OCL-3 cell
-
Homo sapiens
-
REH cell renal carcinoma cells Homo sapiens
-
SU.86.86 cell pancreatic cancer cells Homo sapiens
-

Synonyms

Synonyms Comment Organism
Topoisomerase I
-
Homo sapiens