Camptothecin resistance

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WebAug 1, 1998 · Recent Food and Drug Administration approval of the camptothecin analog irinotecan (CPT-11 [Camptosar]) for the treatment of colorectal cancer resistant to … WebIn this study, we established an SN-38-resistant cell line, PC-6/SN2-5, from the human oat cell carcinoma PC-6 cell line by a stepwise selection system, investigated the mechanism of resistance of this cell line and then compared the antitumor activity of camptothecin analogs against the cell line.

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WebNázev Camptothecin Přístupové číslo DB04690 Popis. Camptothecin je alkaloid izolovaný ze dřeva kmene čínského stromu Camptotheca acuminata. Tato sloučenina selektivně inhibuje jaderný enzym DNA topoizomerázu typu I. Několik polosyntetických analogů kamptothecinu prokázalo protinádorovou aktivitu. WebSupported by detailed understanding of their mechanism of action, and facilitated by chemical manipulations that have amplified their solubility, the camptothecins have advanced to the forefront of several areas of therapeutic and developmental chemotherapy. Additive and synergistic laboratory interactions with other cytotoxic drugs have been … high five certification online

Single Mutation in the Linker Domain Confers Protein …

WebObjective: To determine the prognostic role of a K-ras mutation in tumor tissue of patients with refractory colon cancer who received irinotecan hydrochloride (CPT-11). Methods: DNA was extracted from paraffin-stored tumor tissue of 35 patients with progressive colon cancer failing treatment with 5-fluorouracil who subsequently received CPT-11 (100 mg/m2 i.v. … WebThe mechanisms of resistance to CPT-11 in PC-7/CPT-11 cells were reduced conversion of CPT-11 to its active metabolite SN-38 and point mutation of topoisomerase I. Those in HAC-2/CPT-11 cells were reduction of topoisomerase I activity and decreased sensitivity of topoisomerase to topoisomerase I inhibitors. WebOct 2, 2001 · Abstract. From the rat C6 glioma cell line in culture, we selected camptothecin-resistant variants by growth in the presence of increasing amounts of … how hotwire a car

Camptothecin Sensitivity Is Mediated by the Pleiotropic Drug Resistance ...

Camptothecin: Biosynthesis, Biotechnological Production and Resistance ...

WebSep 16, 2024 · This suggests that G363C and G737S mutations had only slight effects on CPT resistance. On the basis of these results, we set the concentration of CPT and Genz for further analysis as 10 μM... WebMay 6, 2008 · We found that CPT-producing plants, including Camptotheca acuminata, Ophiorrhiza pumila, and Ophiorrhiza liukiuensis, have Top1s with point mutations that confer resistance to CPT, suggesting the effect of an endogenous toxic metabolite on the evolution of the target cellular component. high five chatWebJan 1, 2001 · The resistance ratio to CPT was >2000 fold. Western blot analysis using monoclonal antibody against top1 does not detect top1 in P388/CPT45. This cell line was used recently to show that the top1 inhibition might contribute to the antiproliferative activity of 1-β- d -arabinofuranosylcytosine (12). how houdini accomplished

"WebDec 31, 2013 · Camptothecin (CPT) is a kind of quinoline alkaloid that has gained great attention due to its unique anti-tumor activities . Two semi-synthetic water-soluble … " - Camptothecin resistance

Camptothecin resistance

Use of Camptothecin-resistant Mammalian Cell Lines to Evaluate …

WebDec 16, 2024 · Camptothecin derivatives are precursors of potent anticancer agents, but their biosynthesis remains largely unknown. ... D. et al. Induction of multiple pleiotropic drug resistance genes in yeast ...

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WebApr 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 … WebCamptothecin complexes with type I DNA topoisomerase inhibiting both cleavage and religation reactions of DNA replication thus arresting growth of L. donovani …

WebOct 14, 2024 · (±)-Hypersines A–C (1–3), the three pairs of enantiomerically pure monoterpenoid polyprenylated acylphloroglucinols with an unprecedented 6/6/5/4 fused ring system, were isolated from Hypericum elodeoides. Their structures, including absolute configurations, were elucidated by comprehensive spectroscopic data, single-crystal X … WebJan 1, 2013 · Camptothecin (CPT) is a water insoluble and cytotoxic monoterpene indole alkaloid, which is used as the substrate to form water-soluble derivatives (such as …

Studies have shown that substitution at position 7, 9, 10 and 11 can have positive effect on CPT activity and physical properties, e.g. potency and metabolic stability. Enlargement of the lactone ring by one CH 2 unit also enhances its abilities, as in homocamptothecin. Substitution at position 12 and 14 leads to inactive derivative. WebDec 31, 2013 · Camptothecin (CPT) is a water-insoluble tryptophan-derived quinolone alkaloid and is a lead compound for two FDA (Food and Drug Administration) approved antineoplastic drugs, irinotecan and...

WebDec 1, 1999 · The present study describes camptothecin resistance and the potential for drug glucuronidation in two cell lines overexpressing the ABC half-transporter, …

WebApr 28, 2015 · Irinotecan is a camptothecin analogue currently used in clinical practice to treat advanced colorectal cancer. However, acquired resistance mediated by the drug efflux pump ABCG2 is a recognized problem. We reported on a novel camptothecin analogue, FL118, which shows anticancer activity superior to irinotecan. how hou move the.cow in conker bad fer dayWebJan 10, 2024 · As camptothecin resistance in cancer is common, it will be interesting to test if p97 inhibition might also restore the cytotoxicity of camptothecin and prolong its efficacy. In summary,... high five chicken hastingsWebNov 7, 2015 · Camptothecin resistance is determined by the regulation of topoisomerase I degradation mediated by ubiquitin proteasome pathway.pdf Available via license: CC BY 3.0 Content may be subject to ... how hot will it get todayWebJul 1, 2024 · Abstract. Proteasomal degradation of topoisomerase I (topoI) is one of the most remarkable cellular phenomena observed in response to camptothecin (CPT). Importantly, the rate of topoI degradation is linked to CPT resistance. Formation of the topoI-DNA-CPT cleavable complex inhibits DNA re-ligation resulting in DNA-double … high five chickenWebMar 31, 2016 · DNA topoisomerase I (Top1) is a DNA unwinding protein and the specific target of the camptothecin class of chemotherapeutic drugs. One of these, irinotecan, acting through its active metabolite SN-38, is used in the treatment of metastatic colorectal cancer. However, resistance to irinotecan represents a major clinical problem. Since … high five chocolateWebBenedetti P, Fiorani P, Capuani L, Wang JC. 1993 Camptothecin resistance from a single mutation changing glycine 363 of human DNA topoisomerase I to cysteine. Cancer Res … high five chicken langleyWebJul 4, 2024 · Camptothecin resistance is determined by the regulation of topoisomerase I degradation mediated by ubiquitin proteasome pathway. Proteasomal degradation of … high five chicken burnaby