Protein Variants | Comment | Organism |
---|---|---|
E710G | site-directed mutagenesis, the mutation is not detectable in tissue samples from colorectal cancer patients | Homo sapiens |
L617I | site-directed mutagenesis, the mutation is not detectable in tissue samples from colorectal cancer patients | Homo sapiens |
R621H | site-directed mutagenesis, the mutation is not detectable in tissue samples from colorectal cancer patients | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
camptothecin | - |
Homo sapiens | |
irinotecan | i.e. CPT-11, a derivative of camptothecin and an anticancer agent in the treatment of metastatic colon cancer | Homo sapiens | |
SN38 | enzyme linker fluctuations can have an impact on SN38 binding by reducing the enzyme affinity for the drug. TOP1 mutations are involved in the development of SN38 resistance | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
nucleus | - |
Homo sapiens | 5634 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | the enzyme catalyzes the relaxation of supercoiled DNA during DNA replication and transcription | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
HCT-116 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | the enzyme catalyzes the relaxation of supercoiled DNA during DNA replication and transcription | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Top1 | - |
Homo sapiens |
Topoisomerase I | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
malfunction | TOP1 mutations are involved in the development of SN38 resistance. Mutation of one of residues L617, R621, and E710, important for the functionality of the linker, is sufficient to alter or modulate its flexibility. DNA double strand break formation is reduced in SN38 resistant HCT116 cells. Colorectal cancer patients and SN38 resistant HCT116 clones phemotypes, overview | Homo sapiens |
additional information | residues L617, R621, and E710 are important for the functionality of the linker in the enzyme | Homo sapiens |