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. 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 …
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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 … 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.
WebJun 13, 2024 · Nonetheless, applications of camptothecin are limited by water insolubility, rapid conversion of its bioactive lactone form to inactive carboxylate under physiological conditions, drug resistance and off-target side effects. Here, we review the delivery of camptothecin by active and passive targeting for anticancer activity. 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 …
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... 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.
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 …
WebNational Center for Biotechnology Information great clips specialsWebMay 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. great clips speedway hoursWebObjective: 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. … great clips special offerWebSep 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... great clips speedway inWebMay 13, 2015 · In continuation of our program aimed at the development of natural product-based pesticidal agents, three series of novel camptothecin derivatives were designed, synthesized, and evaluated for their biological activities against T. Cinnabarinus, B. brassicae, and B. xylophilus. All of the derivatives showed good-to-excellent activity … great clips speedway plazaWebApr 10, 2024 · The virtual screening revealed that two alkaloidal metabolites, camptothecin and GKK1032A2 showed excellent binding energy with any target proteins compared to reference commercial fungicides, Azoxystrobin and Strobilurin. ... However, extensive use of chemical fungicides has resulted in development of resistance in fungus against the ... great clips speedwayWebDec 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 ... great clips speedway indiana