Camptothecin resistance

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August undefined, 2024

WebApr 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 ... 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 …

Camptothecin: Biosynthesis, Biotechnological Production …

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 … 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 … csm christopher carey

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

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 … 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). 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,... csm chris mullinax

Camptothecin resistance is determined by the regulation …

Camptothecin Sensitivity Is Mediated by the Pleiotropic Drug …

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. WebNational Center for Biotechnology Information csm chris fieldsWebApr 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 … csm christian

"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. … " - Camptothecin resistance

Camptothecin resistance

Camptothecin - an overview ScienceDirect Topics

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. 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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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. 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 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 ... 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.

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

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 ...

eagle senior living corporate officeWebAug 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. csm christopher goodartWebMay 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. csm christopher gunnWebDec 1, 2024 · Camptothecin discovery and early development. Camptothecin (CPT) (Figure 1A) is a pentacyclic alkaloid that was first isolated from stem wood of Camptotheca acuminata by botanists working in the USDA’s Plant Introduction Division in the mid-1950s [].Camptotheca acuminata is a tree native to China and its bark is a recognized Chinese … csm christopher d. clapinWebMay 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 … eagle senior golf group knoxvilleWebOct 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. eagle series by drive f-22 costWebOct 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 … eagle series by drive f22 rollator