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Literature summary for 5.6.2.1 extracted from

  • Koster, D.A.; Palle, K.; Bot, E.S.; Bjornsti, M.A.; Dekker, N.H.
    Antitumour drugs impede DNA uncoiling by topoisomerase I (2007), Nature, 448, 213-217.
    View publication on PubMed

Application

Application Comment Organism
drug development topoisomerase–drug interactions for clinical development of chemotherapeutics Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
Saccharomyces cerevisiae strains EKY2 (MATa, top1D) and EKY3(MATa, top1D) Homo sapiens

Protein Variants

Protein Variants Comment Organism
G365C camptothecin-resistant Top1(G365C) mutant Homo sapiens
Y723F catalytically inactive TOP1(Y723F) Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
camptothecin Camptothecin poisoning of TopIB induces accumulation of positively supercoiled DNA in G1- and S-phase yeast cells. Mechanism of camptothecin-induced toxicity derives from TopIB-dependent accumulation of positive supercoils Homo sapiens
topotecan Camptothecin analogue, induce cell death by poisoning DNA topoisomerase I, topotecan significantly hinders topoisomerase-mediated DNA uncoiling, with a more pronounced effect on the removal of positive (overwound) versus negative supercoils. Significant activity against adult and paediatric solid tumours Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Synonyms

Synonyms Comment Organism
DNA topoisomerase I
-
Homo sapiens
TopIB
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Homo sapiens
Topoisomerase I
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Homo sapiens