Camptothecin resistance

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... 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.

Mechanism of action of non-camptothecin inhibitor Genz-644282 …

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 … WebCamptothecin complexes with type I DNA topoisomerase inhibiting both cleavage and religation reactions of DNA replication thus arresting growth of L. donovani … china reserve securities limited https://heppnermarketing.com

IJMS Free Full-Text Quantitative Evaluation of Drug Resistance ...

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. 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. 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 … china reserve military size

Topoisomerase I inhibitors: camptothecins and beyond

Category:Camptothecin: Uses, Interactions, Mechanism of Action

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Camptothecin resistance

Camptothecin: Uses, Interactions, 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 … 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 …

Camptothecin resistance

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

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 … 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.

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 … 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.

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 …

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. … china re share priceWebMar 31, 2016 · DNA topoisomerase I (Top1) is a DNA unwinding protein and the specific target of the camptothecin class of chemotherapeutic drugs. One of these, irinotecan, acting through its active metabolite SN-38, is used in the treatment of metastatic colorectal cancer. However, resistance to irinotecan represents a major clinical problem. Since … china residential earthquake insurance poolWebmultidrug 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 china residential ev chargerWebDec 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 ... china residential property market 2021WebNázev 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. grammarly checker online grammarWebAug 1, 1998 · Recent Food and Drug Administration approval of the camptothecin analog irinotecan (CPT-11 [Camptosar]) for the treatment of colorectal cancer resistant to … china residence registration formWebJan 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. china residence permit renewal