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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Synonyms | Comment | Organism |
---|---|---|
DNA topoisomerase I | - |
Homo sapiens |
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 |