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sup][18] To the best of our knowledge, no report has elucidated the role of deoxyribonucleic acid (DNA) topoisomerase I inhibitors in cancer-initiating cells.
Altered topoisomerase I expression in two subclones of human CEM leukemia selected for resistance to camptothecin.
Camptothecins with their docking score of their antineoplatic, topoisomerase I inhibitory, DNA intercatalor activity are shown in Tables 1,2 and 3.
In preclinical studies XR11576 has shown a significantly improved biological profile when compared with first generation dual topoisomerase I and II inhibitors, including oral bioavailability and a marked enhancement of potency.
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.
The agent works by inhibiting the topoisomerase I enzyme that is essential for cell division.
Nasdaq: OSIP) today announced the initiation of two Phase II clinical trials of OSI-211, an investigational liposomal formulation of the potent topoisomerase I inhibitor lurtotecan.
In addition, a large body of preclinical evidence shows a synergistic cytotoxic interaction between topoisomerase I inhibitors similar to irinotecan, and irofulven.