1246194-65-9Relevant academic research and scientific papers
Taxol-DHA-dextran coupling polymer, synthetic method thereof and application of polymer
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, (2019/10/01)
The invention provides a taxol-DHA-dextran coupling polymer, a synthetic method thereof and an application of the polymer, and belongs to the technical field of biological medicines. According to thepolymer, polysaccharides serve as polymer drug-loaded frameworks, so that an anti-tumor drug-polysaccharide passive targeted coupling polymer is prepared, taxol can be passively targeted into a tumortissue by the aid of an EPR effect, and an anti-tumor function is played. Water solubility and biocompatibility of taxol medicines can be increased, accumulation of anti-tumor medicines in the tumor tissue can be increased under the passive targeted action, general side effect and nervous side effect of the taxol medicines are reduced, and the polymer has good practical application values.
Design, synthesis and bioevaluation of an EphA2 receptor-based targeted delivery system
Barile, Elisa,Wang, Si,Das, Swadesh K.,Noberini, Roberta,Dahl, Russell,Stebbins, John L.,Pasquale, Elena B.,Fisher, Paul B.,Pellecchia, Maurizio
, p. 1403 - 1412 (2014/07/21)
Because of its overexpression in a range of solid tumors, the EphA2 receptor is a validated target for cancer therapeutics. We recently described a new targeted delivery system based on specific EphA2-targeting peptides conjugated with the chemotherapeutic agent paclitaxel. Here, we investigate the chemical determinants responsible for the stability and degradation of these agents in plasma. Introducing modifications in both the peptide and the linker between the peptide and paclitaxel resulted in drug conjugates that are both long-lived in rat plasma and that markedly decrease tumor size in a prostate cancer xenograft model compared with paclitaxel alone treatment. These studies identify critical rate-limiting degradation sites on the peptide-drug conjugates, enabling the design of agents with increased stability and efficacy. These results provide support for our central hypothesis that peptide-drug conjugates targeting EphA2 represent an innovative and potentially effective strategy to selectively deliver cytotoxic drugs to cancer cells. Ready, aim, fire! We investigated the chemical determinants responsible for the stability and degradation in plasma of an EphA2-based targeted delivery system that is constituted by receptor-targeting peptides conjugated with paclitaxel. We demonstrate that our agents are both long-lived in plasma and markedly decrease tumor size in a prostate cancer xenograft model.
Novel targeted system to deliver chemotherapeutic drugs to EphA2-expressing cancer cells
Wang, Si,Placzek, William J.,Stebbins, John L.,Mitra, Sayantan,Noberini, Roberta,Koolpe, Mitchell,Zhang, Ziming,Dahl, Russell,Pasquale, Elena B.,Pellecchia, Maurizio
, p. 2427 - 2436 (2012/05/31)
The efficacy of anticancer drugs is often limited by their systemic toxicities and adverse side effects. We report that the EphA2 receptor is overexpressed preferentially in several human cancer cell lines compared to normal tissues and that an EphA2 targeting peptide (YSAYPDSVPMMS) can be effective in delivering anticancer agents to such tumors. Hence, we report on the synthesis and characterizations of a novel EphA2-targeting agent conjugated with the chemotherapeutic drug paclitaxel. We found that the peptide-drug conjugate is dramatically more effective than paclitaxel alone at inhibiting tumor growth in a prostate cancer xenograft model, delivering significantly higher levels of drug to the tumor site. We believe these studies open the way to the development of a new class of therapeutic compounds that exploit the EphA2 receptor for drug delivery to cancer cells.
