WebJul 12, 2024 · Prodrug–prodrug activation Camptothecin 4 is a topoisomerase I inhibitor that induces S-phase specific cell death. Since its discovery in the 1960's, several camptothecin derivatives and prodrugs have been reported with the aim of overcoming the drawbacks associated with camptothecin such as solubility and the stability of the … WebSep 11, 2007 · Camptothecin is an alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata. This compound selectively inhibits the nuclear enzyme …
Synthesis and activity of a folate peptide camptothecin prodrug
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 … 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 … phillip rentals
Prodrugs: design and clinical applications - Nature
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 ). WebOct 21, 2024 · A camptothecin prodrug induces mitochondria-mediated apoptosis in cancer cells with cascade activations. Mitochondria are crucial regulators of the … WebAbstract 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. try spinning thats a neat trick