Irinotecan topoisomerase 1 inhibitor
WebAbstract. Topotecan and irinotecan (CPT-11) are both anticancer agents active in the inhibition of topoisomerase I, an enzyme involved in DNA replication and RNA … WebTopoisomerase I inhibitors represent a widely used class of antineoplastic agents that promote both single-stranded and double-stranded breaks in the DNA of tumor cells, leading to tumor cell death. Topotecan and irinotecan are the clinically relevant derivatives of the parent drug, camptothecin. As is the case with many if not most anticancer ...
Irinotecan topoisomerase 1 inhibitor
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WebIrinotecan (CPT-11, (+)-Irinotecan) is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. CAS No. 97682-44-5 Selleck's Irinotecan (CPT-11) has been cited by publications Cell Death Dis,202414 (1):64 Cancers (Basel),202414 (5)1230 Oncotarget,202413:1094-1108 Cell Death Discov,20248 (1):296 WebIrinotecan (CPT-11) is topoisomerase I inhibitor used in the treatment of disseminated colorectal cancer. In colon cancer cells it induces DNA damage which leads to cytotoxicity with ensuing apoptosis or premature senescence. Despite its clinical use and efficiency in malignant colonocytes, its effects in normal colonic cells are relatively ...
WebThis medication is classified as a "topoisomerase 1 inhibitor." (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. Topotecan may also be used in certain types of lung cancer (small cell lung cancer). ... WebJul 31, 2024 · Topoisomerase I inhibitor, irinotecan, depletes regulatory T cells and up-regulates MHC class I and PD-L1 expression, resulting in a supra-additive antitumor …
WebA. Alfirevic, M. Pirmohamed, in Medical and Health Genomics, 2016 Topoisomerase I Inhibitors. Irinotecan, used in colorectal cancer, is bioactivated into SN-38 by carboxyesterases 1 and 2 and then bioinactivated by glucuronidation via uridine diphosphate glucuronosyltransferase isoform 1A1 (UGT1A1).The variable number of tandem repeat … WebNov 22, 2011 · The topoisomerase I (Top 1) poison irinotecan is an important component of the modern treatment of colorectal cancer. By stabilising Top 1-DNA complexes, …
Webmer conjugate of irinotecan, a topoisomerase 1 (Top1) inhibitor, designed to provide continuous exposure of SN38 in tumors while avoiding high irinotecan and SN38 plasma concentrations that lead to high AUCs associated with unwanted side effects [10]. Etirinotecan pegol uses propri-etary polymer conjugation with large-chain polyethylene
WebThe anticancer agent, irinotecan, is a prodrug that is converted by tissue carboxylesterase to 7-ethyl-10-hydroxycamptothecin (SN-38), a potent inhibitor of DNA topoisomerase I. Its action is terminated by glucuronidation by UDP glucuronosyl transferase. Safety Information Pictograms GHS07 Signal Word Warning Hazard Statements H302 images uterus and ovariesWebDec 1, 1997 · Abstract. Topoisomerase I inhibitors are a new class of anticancer agents with a mechanism of action aimed at interrupting DNA replication in cancer cells, the result of … images valley of flowersWebFeb 13, 2024 · Irinotecan (SN-38) is a potent and broad-spectrum anticancer drug that targets DNA topoisomerase I (Top1). It exerts its cytotoxic effects by binding to the Top1 … images vaticanWebIrinotecan (CPT-11), a prodrug for treating metastatic colorectal cancer, is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively … images ventral herniaWebAn anthracycline topoisomerase II inhibitor used as an adjuvant to treating axillary node metastases in patients who have undergone surgical resection of primary breast cancer. ... Irinotecan: DNA topoisomerase 1: target: Irinotecan: Cytochrome P450 3A4: enzyme: Irinotecan: Cytochrome P450 3A5: enzyme: Irinotecan: UDP-glucuronosyltransferase 1 ... images velvet lined jewelry traysWebTopoisomerase inhibitors block the ligation step of the cell cycle, which generates DNA single- ... images vaginal yeast infectionWebFeb 13, 2024 · Irinotecan (SN-38) is a potent and broad-spectrum anticancer drug that targets DNA topoisomerase I (Top1). It exerts its cytotoxic effects by binding to the Top1-DNA complex and preventing the re-ligation of the DNA strand, leading to the formation of lethal DNA breaks. Following the initial response to irinotecan, secondary resistance is … images venus williams