Camptothecin resistance

Author: tigo

August undefined, 2024

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. 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 ...

Mutations in topoisomerase I as a self-resistance mechanism ... - PNAS

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

LWJ-M30, a conjugate of DM1 and B6, for the targeted therapy of ...

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 … 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. 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. florida chapter of young people\u0027s aa

Camptothecin: Biosynthesis, Biotechnological Production and Resistance ...

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. 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... florida chapter of the iaaoWebSep 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]. great value boom boom shrimp sauce 10 5 oz

"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. " - Camptothecin resistance

Camptothecin resistance

Topoisomerase I inhibitors: camptothecins and beyond

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 … 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 …

Did you know?

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

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 … 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).

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 … 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

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 …

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 … florida chapter 33 inmate propertyWebOct 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. great value boneless smoked hamWebmultidrug 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 great value boom boom sauceWebCamptothecins 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. great value bone brothWebDec 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 ... florida charged as adultWebDec 1, 1999 · The present study describes camptothecin resistance and the potential for drug glucuronidation in two cell lines overexpressing the ABC half-transporter, … florida charged for auto repair not doneWebCamptothecin 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 … florida chapter 490