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• W2468499096 abstract "Clinically ineffective transplatin is highly potent against cancer cells when transformed into a transplatin(IV) prodrug nanoparticle. Herein, a hydrophobic transplatin(IV) was synthesized by H2O2-oxidization of transplatin and attachment of two hydrophobic aliphatic chains. Transplatin(IV) was subsequently encapsulated by a biodegradable amphiphilic copolymer, MPEG-PLA, forming a well-defined spherical micelles (M(TransPt)). Transplatin(IV) was protected efficiently and could be released under a simulated cancerous intracellular condition. Compared to the cisplatin and transplatin, M(TransPt) showed the highest Pt uptake and a clathrin-dependent endocytosis pathway. Most importantly, M(TransPt) displayed a nanomolar IC50 on A2780 cells and a great potency on cisplatin resistant A2780DDP cell line. Overall, this nanoplatform for delivering trans-geometry platinum(IV) drug exhibits excellent characteristics for enhancing efficacy and overcoming cisplatin drug resistance, and holds a strong promise for clinical use in the near future." @default.
• W2468499096 created "2016-07-22" @default.
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• W2468499096 date "2016-07-14" @default.
• W2468499096 modified "2023-10-14" @default.
• W2468499096 title "Turning Ineffective Transplatin into a Highly Potent Anticancer Drug via a Prodrug Strategy for Drug Delivery and Inhibiting Cisplatin Drug Resistance" @default.
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• W2468499096 doi "https://doi.org/10.1021/acs.bioconjchem.6b00302" @default.
• W2468499096 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27380489" @default.
• W2468499096 hasPublicationYear "2016" @default.
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