WebCompounds 9-12 were potent topoisomerase II inhibitors, with 50% inhibitory concentrations (IC(50))ranging from 10 to 40 microM. The cytotoxicity of the compounds … Webirinotecan, a topoisomerase I inhibitor in use for the treatment of cancer patients with BRCA1 mutations (Kennedy et al, 2004), and disulfiram, an aldehyde dehydrogenase inhibitor used in the clinic as an alcohol deterrent. Our group has recently characterised disulfi-ram as an agent specifically toxic to BRCA1/2-deficient cells and
The DNA-topoisomerase Inhibitors in Cancer Therapy
Topoisomerase inhibitors are chemical compounds that block the action of topoisomerases, which are broken into two broad subtypes: type I topoisomerases (TopI) and type II topoisomerases (TopII). Topoisomerase plays important roles in cellular reproduction and DNA organization, as they mediate the cleavage of single and double stranded DNA to relax supercoils, untangle catenanes, and condense chromosomes in eukaryotic cells. Topoisomerase inhibitors i… WebDrug type: Topotecan is an anti-cancer ("antineoplastic" or "cytotoxic") chemotherapy drug. This medication is classified as a "topoisomerase (For more detail, see "How this drug works" section below). What Topotecan Is Used For: This medicine is used to treat cancer of the ovaries when other treatments have failed. graphing derivatives worksheet with answers
DNA topoisomerases as molecular targets for anticancer drugs
WebTopoisomerase inhibitors are used to treat certain leukemias, as well as lung, ovarian, gastrointestinal, colorectal, and pancreatic cancers. Topoisomerase inhibitors are … WebOct 15, 2007 · It is used to treat a number of forms of cancer such as ovarian cancer, lung cancer, brain cancer, and neuroblastoma. Whereas, oxaliplatin was patented in 1976 and approved in 1996 for its medical use. It is used for treatment of colorectal cancer. Sign in to download full-size image Fig. 19.8. Structures of carboplatin, cisplatin, oxaliplatin. b. WebThe progenitor of topoisomerase I inhibitors is the natural pentacyclic alkaloid camptothecin (CPT), isolated from the Camptotheca acuminata tree (20-22). Although its discovery dates back to the 1960s, the identification of this molecule as an anticancer agent is much more recent. chirping inmate sales