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Literature summary for 5.6.2.1 extracted from

  • Gongora, C.; Vezzio-Vie, N.; Tuduri, S.; Denis, V.; Causse, A.; Auzanneau, C.; Collod-Beroud, G.; Coquelle, A.; Pasero, P.; Pourquier, P.; Martineau, P.; Del Rio, M.
    New topoisomerase I mutations are associated with resistance to camptothecin (2011), Mol. Cancer, 10, 64.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 5.6.2.1

Protein Variants

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

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

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

Natural Substrates/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HCT-116 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
Top1
-
 Homo sapiens
Topoisomerase I
-
 Homo sapiens

General Information

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