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Literature summary for 5.6.2.1 extracted from

  • Capranico, G.; Marinello, J.; Baranello, L.
    Dissecting the transcriptional functions of human DNA topoisomerase I by selective inhibitors: implications for physiological and therapeutic modulation of enzyme activity (2010), Biochim. Biophys. Acta, 1806, 240-250.
    View publication on PubMed
Search for more literature for 5.6.2.1

Inhibitors

Inhibitors Comment Organism Structure
(5Z,7E,9E,14Z,17Z)-icosa-5,7,9,14,17-pentaenoic acid
-
 Homo sapiens
2'-(4-ethoxyphenyl)-6-(4-methylpiperazin-1-yl)-1H,3'H,2,5'-bisbenzimidazole Hoechst 33342 Homo sapiens
4-[5-(4-methyl-1-piperazinyl)-1H,1H'-2,5'-bibenzimidazol-2'-yl]phenol Hoechst 33258 Homo sapiens
9-aminoacridine acts as Top1 poison Homo sapiens
batracylin
-
 Homo sapiens
beta-lapachone
-
 Homo sapiens
bulgarein stabilize inactive Top1cc Homo sapiens
calothrixins weak inhibitors of Top1 Homo sapiens
camptothecin a selective inhibitor of DNA topoisomerase I. Camptothecin activates the transcription of low-abundance antisense RNAs at the HIF-1alpha gene locus in human cancer cells in a topoisomerase I-dependent manner, likely due to sustained drug interference with transcription regulation mechanisms leading to a more open chromatin conformation and de-repression/activation of antisense transcription. Top1cc is then a specific DNA damage induced by the drug, damage and repair mechanisms, detailed overview Homo sapiens
coralyne potent and selective Top1 inhibitor Homo sapiens
diospyrin promotes protein conformational changes that can affect the kinase activity of Top1 altering SR protein phosphorylation and alternative splicing Homo sapiens
edotecarin
-
 Homo sapiens
erybraedin C binds irreversibly to the enzyme alone, probably in proximity of the active site, without abolishing enzyme binding to the DNA Homo sapiens
fagaronine
-
 Homo sapiens
indotecan
-
 Homo sapiens
irinotecan a prodrug and it is activated by hydrolysis to the biologically active metabolite SN-38 Homo sapiens
lamellarin D stabilize inactive Top1cc Homo sapiens
additional information the benz[a]acridine analogues, noncharged bioisosteres of protoberberine alkaloids, are also Top1 inhibitors Homo sapiens
nitidine
-
 Homo sapiens
plukenetione A can inhibit the unwinding activity of Top1 Homo sapiens
saintopin
-
 Homo sapiens
tafluposide
-
 Homo sapiens
thaspine
-
 Homo sapiens
topopyrone D
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
DNA topoisomerase I
-
 Homo sapiens

General Information

General Information Comment Organism
malfunction enzyme inhibition activates transcriptional Cdk (Cdk9 and/or Cdk7) activity leading o the hyperphosphorylation of the CTD of the largest subunit of RNA polymerase II Homo sapiens
additional information camptothecin is a selective inhibitor of DNA topoisomerase I. Camptothecin activates the transcription of low-abundance antisense RNAs at the HIF-1alpha gene locus in human cancer cells in a Topoisomerase I-dependent manner, likely due to sustained drug interference with transcription regulation mechanisms leading to a more open chromatin conformation and de-repression/activation of antisense transcription Homo sapiens