Camptothecin resistance

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August undefined, 2024

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 … 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 …

Camptothecin resistance is determined by the regulation …

WebJan 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). 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... can mold harm you

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

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 topotecan and irinotecan) for use as anti-cancer drugs. WebJan 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,... Webcamptothecin-resistant. The catalytic and structural dy-namical properties of a human DNA topoisomerase I mutant in which Ala-653 in the linker domain was mu-tated into Pro have been investigated. The mutant is resistant to camptothecin and in the absence of the drug displays a cleavage-religation equilibrium strongly shifted toward religation. fix folder icons windows 10

RCSB PDB - 1RR8: Structural Mechanisms of Camptothecin …

Camptothecin - an overview ScienceDirect Topics

WebSep 11, 2007 · Camptothecin demonstrated strong anticancer activity in preliminary clinical trials but also low solubility and adverse drug reaction. Camptothecin is believed to be a potent topoisomerase inhibitor that interferes with the essential function of topoisomerase in DNA replication. Mechanism of action WebApr 14, 2005 · Transfection of Bcl-2 into A549 cells induced a resistance to the short-term apoptotic effect triggered by 12459, suggesting that Bcl-2 is an important determinant for the activity of 12459. ... In contrast, the G-overhang degradation was not observed when apoptosis was induced by camptothecin. Bcl-2 overexpression did not modify the G … can mold harm humans or other animalsWebObjective: 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. … can mold grow without air

"WebSep 11, 2007 · Camptothecin demonstrated strong anticancer activity in preliminary clinical trials but also low solubility and adverse drug reaction. Camptothecin is believed to be a … " - Camptothecin resistance

Camptothecin resistance

Camptothecin Radiation Sensitization: Mechanisms, Schedules, …

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. Webmultidrug resistance, MDR 烷化剂(氮芥、乙撑亚胺类) G1 / S期, S/G2期, G2 /M期存在调控机制真核细胞拓扑结构由拓扑异构酶Ⅰ和Ⅱ调节,维持DNA复制、转录修复、形成正确染色体结构对正常组织细胞也有损伤 – 化疗时用量受限的关键因素 • 肿瘤细胞产生耐药性

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

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... WebJul 4, 2024 · Camptothecin resistance is determined by the regulation of topoisomerase I degradation mediated by ubiquitin proteasome pathway. Proteasomal degradation of …

WebBenedetti 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 … WebJul 4, 2024 · Broad-spectrum resistance in cancer cells is often caused by the overexpression of ABC transporters; which varies across individuals because of genetic single-nucleotide polymorphisms (SNPs). In the present study; we focused on human ABCC4 and established cells expressing the wild-type (WT) or SNP variants of human …

WebDec 5, 2024 · The highly toxic payloads, for instance, maytansine, camptothecin derivatives, auristatin, or doxorubicin are recommended to choose in the conjugates. 9 Finally, ... At the same time, the drug resistance, the recurrence and metastasis of cancer still seriously threaten the health of the patients. 34 Therefore, it is urgent to design highly ...

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. fix footer on mobileWebDec 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 ... can mold humidifiers make you sickWebCamptothecins are broad-spectrum anticancer drugs that specifically target DNA topoisomerase I. Although the availability of camptothecins has had a significant impact on cancer therapeutics, de novo or acquired clinical resistance to camptothecins is common. fix folding chairWebApr 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 … fix footer to bottomWebJan 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 … fix folding door trackWebIn 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. fixfootWebAug 1, 1998 · Recent Food and Drug Administration approval of the camptothecin analog irinotecan (CPT-11 [Camptosar]) for the treatment of colorectal cancer resistant to fluorouracil (5-FU) [1] has opened a new chapter in chemotherapeutic radiation sensitization. can mold harm cats