Camptothecin prodrug

WebNov 14, 2003 · Abstract. 7-Ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (irinotecan, CPT-11) is a camptothecin prodrug that is metabolized by carboxylesterases (CE) to the active metabolite 7-ethyl-10-hydroxycamptothecin (SN-38), a topoisomerase I inhibitor. CPT-11 has shown encouraging antitumor activity against a broad spectrum of … WebJan 13, 2024 · Therapeutic conjugate approaches that alter the solubility of a conjugate “prodrug” have been used to enable NC formation and controlled release from NCs using labile linker chemistry. A limitation of this approach has been that a different linker chemistry must be used to produce an adjustable release rate for a single therapeutic.

Case Study: Irinotecan (CPT-11), A Water-soluble Prodrug of SN …

WebCamptothecin and lactose act as the chemotherapy drug and targeting ligand in the drug delivery system, respectively. Since CPT-S-S-LA is an amphiphilic compound, it can self-assemble into nanoparticles with a diameter of around 110 nm. The CPT-S-S-LA nanoparticles displayed controllable drug release behavior in the physiological environment. WebCamptothecin (CPT, 1) is a plant alkaloid from the Camptotheca acuminata tree. 83 In in vitro assay, camptothecin exhibited excellent topoisomerase I inhibitory activity but poor … the pa profession https://alistsecurityinc.com

ROS‐Responsive Camptothecin Prodrug Nanoparticles

WebApr 23, 2024 · Herein, a helix self-assembly camptothecin (CPT) prodrug with simultaneous physical and physiological tumor penetration was constructed to realize effective chemo-immunotherapy. Specifically, CPT was modified with arginine to self-assemble into nanofibers to physically improve tumor penetration. WebFeb 16, 2024 · The aim of this study was to prepare small-molecule camptothecin (CPT) prodrugs and evaluate their effectiveness in colorectal carcinoma therapy. Prodrug nanoparticles (NPs) were physicochemically characterized and evaluated for their cytotoxicity in human colon cancer (HCT116) cell lines. The antitumor efficacy of the NPs … WebThe PEG-CPT prodrug is obtained by conjugation of a 40 ... Camptothecin is a natural compound isolated from the plant camptotheca accuminata. The sodium salt of … shuttle from chicago to west lafayette

Activation of a camptothecin prodrug by specific …

Category:Prodrug-Based Versatile Nanomedicine with Simultaneous …

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Camptothecin prodrug

ROS‐Responsive Camptothecin Prodrug ... - Wiley Online …

WebThe clinical efficacy of cytotoxic drugs in the treatment of cancer is often hampered by poor pharmacodynamics and systemic toxicity. Here, we describe the design and synthesis of a new PEG-based system for the delivery of the cytotoxic camptothecin (CPT) into tumor cells that overexpress luteinizing hormone releasing hormone receptor (LHRHR). WebNational Center for Biotechnology Information

Camptothecin prodrug

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WebFeb 28, 2024 · Camptothecin (CPT) is a pentacyclic quinoline alkaloid drug, which possesses superior antitumor efficacy, antiproliferative effect and apoptosis induction capacity in colon, lung, breast, ovarian, melanoma and other cancers. WebNov 28, 2024 · Camptothecin (CPT), a DNA topoisomerase I inhibitor that induces DNA damage in cancer cells, has been widely used for the treatment of a variety of cancers, …

WebDec 31, 2024 · In this paper, galactose decorated trimethyl chitosan (GT)–camptothecin (CPT) prodrug nanoparticles (GT-ss-CPT NPs) were prepared from GT-CPT conjugates linked by dithiodipropionic acid. The obtained GT-ss-CPT NPs were spherical with a particle size of 184.1 nm. GT-ss-CPT NPs displayed low drug release under physiological … WebIrinotecan is a prodrug designed to deliver the poorly soluble parent molecule SN-38, an analog of a highly potent plant alkaloid camptothecin (CPT). Camptothecin and its analogs inhibit the nuclear enzyme topoisomerase I, inhibiting replication and demonstrating antitumor activity as an S-phase-specific drug ( Garcia-Carbonero and Supko, 2002 ).

WebFeb 4, 2024 · Conventional chemotherapy and targeted therapy promote the antitumor immune response by increasing the immunogenicity of tumor cells, improving CD8+ T cell infiltration, or inhibiting immunosuppressive cells in the tumor microenvironment. WebHerein, we fabricated a novel amphiphilic lactose-camptothecin prodrug molecular Lac-SS-CPT which can self-assemble into Lac-SS-CPT glyco-nano prodrug system for GSH …

WebIt is well known that camptothecin (CPT), which inhibits topoisomerase Ⅰ activity, has significant anticancer activity against various solid tumors in vitro. 29, 30 However, the major problem encountered with CPT is its extremely low solubility and side effects, which lead to the failure of clinical treatment. 31 In order to overcome the problem, …

WebKeywords: CPT prodrug, dual responsive, sequential drug release, prostate-specific membrane antigen, ... Li Y, Lin J, Ma J, et al. Methotrexate–camptothecin prodrug nanoassemblies as a versatile nanoplatform for biomodal imaging-guided self-active targeted and synergistic chemotherapy. the paps mansfieldWebA camptothecin prodrug induces mitochondria-mediated apoptosis in cancer cells with cascade activations - Chemical Communications (RSC Publishing) Issue 84, 2024 Previous Article Next Article From the journal: Chemical Communications A camptothecin prodrug induces mitochondria-mediated apoptosis in cancer cells with cascade activations † shuttle from chicago midwayWebCyclosert- camptothecin is a linear, cyclodextrin-based polymer (CDP) and camptothecin (CPT) conjugate. CPT, an alkaloid extract, displays anticancer activity as an inhibitor of … shuttle from cleveland airport to erie paWebAug 31, 2024 · We report a camptothecin (CPT) prodrug that was well formulated in solution and rapidly transformed into long-circulating nanocomplexes in vivo for … shuttle from colville to spokaneWebAbstract A folate receptor targeted camptothecin prodrug was synthesized using a hydrophilic peptide spacer linked to folate via a releasable disulfide carbonate linker. The conjugate was found to possess high affinity for folate receptor-expressing cells and inhibited cell proliferation in human KB cells with an IC 50 of 10 nM. shuttle from cincinnati airportWebEster prodrugs are most often used to enhance the lipophilicity, and thus the passive membrane permeability, of water-soluble drugs by masking charged groups such as carboxylic acids and... the paps of anuWebAug 5, 2024 · Herein, we designed a glutathione (GSH)-responsive camptothecin (CPT) prodrug-based hybrid micellar nanoparticles (siPD-L1@HM-CPT) to achieve … the paps fana