Camptothecin resistance

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August undefined, 2024

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,... WebMay 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 …

Camptothecin resistance is determined by the regulation of ...

WebOct 1, 2006 · Brangi, M. et al. Camptothecin resistance: role of the ATP binding cassette (ABC) half-transporter, mitoxantrone-resistance (MXR), and potential for glucuronidation in MXR-expressing cells. 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. incident in the life of a slave girl 日本語

Mechanisms of resistance to camptothecins - PubMed

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 … 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. 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 inborn error of krebs cycle

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Camptothecin resistance is determined by the regulation …

WebDec 8, 2003 · We present the crystal structures of two camptothecin-resistant forms of human topoisomerase I (Phe361Ser at 2.6A resolution and Asn722Ser at 2.3A … 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 fluorouracil (5-FU) [1] has opened a new chapter in chemotherapeutic radiation sensitization. incident in the life of a slave girl summaryWebNational Center for Biotechnology Information inborn error of metabolism diagnosis

"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 ... " - Camptothecin resistance

Camptothecin resistance

Camptothecin: Biosynthesis, Biotechnological Production …

WebJan 1, 2001 · Abstract. NB-506 is a topoisomerase I (top1) inhibitor in clinical trials. In this study, we used a series of camptothecin (CPT)-resistant cell lines with known top1 … WebCamptothecin stabilizes a covalent enzyme-DNA intermediate that is converted into lethal double strand DNA lesions during S phase of the cell cycle. Yeast SCT1 mutants were …

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WebMay 11, 2016 · Purpose Indenoisoquinolines are non-camptothecin topoisomerase I (TopI) inhibitors that overcome the limitations of camptothecins: chemical instability and camptothecin resistance. Two dosing schedules of the novel indenoisoquinoline, indotecan (LMP400), were evaluated in patients with advanced solid tumors. Methods …

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 ... 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).

WebOct 7, 2016 · The camptothecins are a new class of chemotherapeutic agents which have a novel mechanism of action targeting the nuclear enzyme topoisomerase I. Knowledge of the structure-activity relationships of the parent compound camptothecin has led to the development of effective soluble analogues with manageable toxicities. 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.

WebJul 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 …

WebSep 15, 2000 · Several resistance mechanisms to camptothecin and its derivatives have been described, including mutations in topoisomerase I [1], decreased levels of topoisomerase I [2], and decreased topotecan accumulation in P-glycoprotein-overexpressing cells [3]. inborn error of metabolismWebcamptothecin-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. incident in the middle of nowhereWebJul 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 … inborn error of lipoprotein metabolismWebSupported 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 … incident in the park analysisWebJun 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. incident in the taigaWebJul 4, 2024 · Camptothecin resistance is determined by the regulation of topoisomerase I degradation mediated by ubiquitin proteasome pathway. Proteasomal degradation of … inborn error of metabolism icd 10WebApr 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 … incident in tipton today