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Relevant academic research and scientific papers

Design, synthesis, and evaluation of water-soluble morpholino-decorated paclitaxel prodrugs with remarkably decreased toxicity

Novel water-soluble paclitaxel prodrugs were designed and synthesized by introducing morpholino groups through different linkers. These derivatives showed 400–20,000-times greater water solubility than paclitaxel as well as comparable activity in MCF-7 an

Bioorthogonal Uncaging of Cytotoxic Paclitaxel through Pd Nanosheet-Hydrogel Frameworks

The promising potential of bioorthogonal catalysis in biomedicine is inspiring incremental efforts to design strategies that regulate drug activity in living systems. To achieve this, it is not only essential to develop customized inactive prodrugs and biocompatible metal catalysts but also the right physical environment for them to interact and enable drug production under spatial and/or temporal control. Toward this goal, here, we report the first inactive precursor of the potent broad-spectrum anticancer drug paclitaxel (a.k.a. Taxol) that is stable in cell culture and labile to Pd catalysts. This new prodrug is effectively uncaged in cancer cell culture by Pd nanosheets captured within agarose and alginate hydrogels, providing a biodegradable catalytic framework to achieve controlled release of one of the most important chemotherapy drugs in medical practice. The compatibility of bioorthogonal catalysis and physical hydrogels opens up new opportunities to administer and modulate the mobility of transition metal catalysts in living environs.

Water-soluble heparin-PTX conjugates for cancer targeting

Targeted drug delivery to cancer cells or tumor vasculature is an attractive approach to treating cancer. We here report the synthesis of an anticancer drug conjugate composed of paclitaxel (PTX) and polysaccharide heparin through the reaction of aminated

Synthesis and Biological Evaluation of an isoDGR-Paclitaxel Conjugate Containing a Cell-Penetrating Peptide to Promote Cellular Uptake

Two new Drug Delivery Systems (DDS) cyclo[DKP-isoDGR]-PEG-4-Val-Ala-PTX (2) and cyclo[DKP-isoDGR]-PEG-4-sC18-Val-Ala-PTX (3), containing the cyclo[DKP-isoDGR] integrin ligand and the cytotoxic agent Paclitaxel (PTX), were synthesized to investigate the influence of a PEG-4 chain and of the sC18 cell-penetrating peptide (CPP) on the cellular uptake and the cytotoxicity of the constructs. A “double click-reaction strategy” was planned, to realize the connection of cyclo[DKP-isoDGR] and PTX to the CPP moiety. Anti-proliferative bioassays were performed on the αVβ3-positive U87 human glioblastoma cell line using a short contact time (15 min) followed by draining, washing of the cells, and re-incubation for 72 h. Compound 3 was significantly more potent (IC50=27.6 μM) than compound 2 (IC50>100 μM), and showed a reduced potency loss with respect to PTX (IC50=71 nM).

Polymeric prodrugs and subcutaneous and/or intramuscular administration thereof

The invention relates to new prodrugs of active molecules. These prodrugs allow, in particular, the subcutaneous or intramuscular administration of active molecules of which the subcutaneous or intramuscular administration is problematic or impossible, in

Taxane amphiphilic polymer prodrug capable of realizing reduction responsive release of bulk drugs, and preparation method and applications thereof

The invention relates to a taxane amphiphilic polymer prodrug capable of realizing reduction responsive release of bulk drugs, and a preparation method and applications thereof. The molecule structural formula of the taxane amphiphilic polymer prodrug is

Selenium-containing paclitaxel dimer prodrug polymer nanoparticle and preparation method thereof

The invention belongs to the field of pharmaceutical preparations, and relates to a selenium-containing paclitaxel dimer prodrug polymer nanoparticle and a preparation method thereof. The preparationis a selenium-containing paclitaxel dimer prodrug polymer nano-drug delivery system prepared from a selenium-containing paclitaxel dimer prodrug, a polyethylene glycol-polypolyphenylalanine amphiphilic polymer material, a polypeptide-modified polyethylene glycol-polyphenylalanine amphiphilic polymer material, and the like; the selenium-containing paclitaxel dimer prodrug polymer nano drug deliverysystem. The selenium-containing paclitaxel dimer prodrug is synthesized and encapsulated in the polyethylene glycol-polyphenylalanine amphiphilic polymer materials, by virtue of a special dimer structure, the high-drug-loading polymer nanoparticle0 is prepared, a Se-Se bond is introduced in the synthesis of the dimer prodrug, carrier stability can be effectively improved, and the controllable release of the drug in target cells can be realized; by modification of polypeptide molecules, the breast cancer targeting property of the nanoparticle can be obviously improved, the accumulation of thedrug is improved, and the anti-tumor effect of the drug is improved.

ANTI-CANCER AGENT AND CANCER CELL KILLING METHOD

[Object] An anticancer agent capable of continuously killing cancer cells in a plurality of phases is provided. [Solution] An anticancer agent contains a complex produced by making a metal-salen complex compound, which includes a central metal and (N, N,

Synthesis and biological evaluation of RGD peptidomimetic-paclitaxel conjugates bearing lysosomally cleavable linkers

Two small-molecule-drug conjugates (SMDCs, 6 and 7) featuring lysosomally cleavable linkers (namely the Val-Ala and Phe-Lys peptide sequences) were synthesized by conjugation of the αvβ3-integrin ligand cyclo[DKP-RGD]-CH2NH2 (2) to the anticancer drug paclitaxel (PTX). A third cyclo[DKP-RGD]-PTX conjugate with a nonpeptide "uncleavable" linker (8) was also synthesized to be tested as a negative control. These three SMDCs were able to inhibit biotinylated vitronectin binding to the purified αVβ3-integrin receptor at nanomolar concentrations and showed good stability at pH 7.4 and pH 5.5. Cleavage of the two peptide linkers was observed in the presence of lysosomal enzymes, whereas conjugate 8, which possesses a nonpeptide "uncleavable" linker, remained intact under these conditions. The antiproliferative activities of the conjugates were evaluated against two isogenic cell lines expressing the integrin receptor at different levels: the acute lymphoblastic leukemia cell line CCRF-CEM (αVβ3-) and its subclone CCRF-CEM αVβ3 (αVβ3+). Fairly effective integrin targeting was displayed by the cyclo[DKP-RGD]-Val-Ala-PTX conjugate (6), which was found to differentially inhibit proliferation in antigen-positive CCRF-CEM αVβ3 versus antigen-negative isogenic CCRF-CEM cells. The total lack of activity displayed by the "uncleavable" cyclo[DKP-RGD]-PTX conjugate (8) clearly demonstrates the importance of the peptide linker for achieving the selective release of the cytotoxic payload.

POLYMERIC SYSTEMS AND USES THEREOF IN THERANOSTIC APPLICATIONS

Polymeric systems useful for theranostic applications are disclosed. The polymeric systems comprise a fluorescent or fluorogenic moiety and a therapeutically active agent, each attached to the same or different polymeric moiety. The polymeric systems are designed such that a fluorescent signal is generated in response to a chemical event, preferably upon contacting an analyte (e.g., an enzyme) that is over- expressed in a diseased tissue or organ. Probes useful for inclusion in such polymeric systems, processes of preparing such probes and the polymeric systems, and uses thereof in diagnostic and/or theranostic applications are also disclosed.