[sup] Perturbed DNA topoisomerase I activity can affect fragile-site breakage at the RET oncogene.
A topoisomerase I inhibitor (topotecan) had a tumor-suppressive effect in chemoresistant ovarian cancer-initiating cells.
Liu, "Camp-tothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I," Journal of Biological Chemistry, vol.
Rothenberg, "Topoisomerase I inhibitors: review and update,"
As can be seen from Figure 4, all of the Camptothecins are potent topoisomerase I inhibitors and all of them show this property more 0.781 .
Previous papersdemonstrated that Camptothecins have anticancer activities, scientists mentioned antineoplatic and topoisomerase I inhibitor activity of Camptothecins (12).
As Figure 1, A indicates, the oligonucleotide contains a high-efficiency cleavage site for topoisomerase I. To eliminate the possibility that topoisomerase I was binding to the oligonucleotide to form a complex, 28 units of topoisomerase I from calf thymus were incubated with the [[sup.32]P]-labeled oligonucleotide for 15 minutes at room temperature.
However, based on our results, the following reactions appear to be involved: (1) Hoechst 33342-induced loss of topoisomerase I activity; (2) Hoechst 33342-induced blockade of transcription at the TATA box-binding protein/TATA box element-binding step; (3) Hoechst 33342-induced mitochondrial dysfunction; and (4) intracellular accumulation of E2F-1.
Specificity of anti-Scl70 antibodies in scleroderma: increased sensitivity of detection using purified DNA topoisomerase I
from calf thymus.
Evodiamine stabilizes topoisomerase 1-DNA cleavable complex to inhibit topoisomerase I
A series of assays for target-specific pharmacodynamic biomarkers for etirinotecan pegol, including the molecular target topoisomerase I
, have been established and are being assessed in the study.
16 November 2011 - Nektar Therapeutics (NASDAQ:NKTR) announced on Tuesday positive results of its preclinical trials of NKTR-102, a topoisomerase I
inhibitor, at the 2011 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer that is currently underway in San Francisco.