5254-51-3

Upstream product

• 75-44-5 phosgene 
• 29456-09-5 L-glutamic acid γ-benzyl ester 
• 617-65-2 Glutamic acid 
• 100-51-6 benzyl alcohol 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 1676-73-9 L-glutamic acid γ-benzyl ester 
• 63228-51-3 L-aspartic acid beta-benzyl ester 
• 3283-43-0 γ-benzyl glutamic acid 
• 1676-73-9 glutamic acid γ-benzyl ester 
• 13574-13-5 Boc-Glu(OBzl)-OH 
• 62457-19-6 N-benzyloxycarbonyl-glutamic acid 5-benzyl ester 1-tert-butyl ester 

Relevant academic research and scientific papers

Biodegradable supramolecular micellesviahost-guest interaction of cyclodextrin-terminated polypeptides and adamantane-terminated polycaprolactones

Biodegradable supramolecular micelles were prepared exploiting the host-guest interaction of cyclodextrin and adamantane. Cyclodextrin-initiated polypeptides acted as the hydrophilic corona, whereas adamantane-terminated polycaprolactones served as the hydrophobic core.

Preparation method and application of folic acid-targeted dual-drug-loaded nanoparticles

The invention relates to a preparation method and application of folic acid-targeted dual-drug-loaded nanoparticles, and can effectively solve problems that anti-tumor drugs are low in water solubility, serious in toxic and side effects, lack of targeting, etc. A technical solution is to prepare dendrimers PLD and polyglutamic acid (PGA), and paclitaxel, gemcitabine and folic acid are loaded on the PGA to obtain PGA-PTX, PGA-GEM and PGA-FA. The four materials in an aqueous solution are attracted to each other by positive and negative charges, and self-assembled to form the nanoparticles, and particle diameters of the nanoparticles are about (190 plus or minus 15) nm. The nanoparticles enter tumor cells and release the paclitaxel and the gemcitabine through combination of the folic acid andfolic acid receptors on surfaces of the tumor cells, thereby inhibiting proliferation of the tumor cells and promoting apoptosis. The drug-loaded nanoparticles can effectively inhibit growth of tumorcells 4T1 and have a better inhibitory effect on tumor models of the 4T1 cells in vivo.

Nano-cluster for treating cancer and preparation method of nano-cluster

The invention relates to the technical field of polymer drug carriers, and in particular relates to a nano-cluster for treating cancer and a preparation method of the nano-cluster. The preparation method includes the following steps: A) performing a reaction on a first mixed liquid and a second mixed liquid to obtain a product solution, wherein the first mixed liquid includes polyamino acid nanoparticles loaded with cisplatin, sodium phosphate, sodium chloride, N-(2-hydroxyethyl)piperazin-N'-2-ethanesulfonic acid and water, and the second mixed solution includes arsenic trioxide, calcium chloride and water; and B) performing dialysis on the product solution, and performing lyophilization to obtain the nano-cluster for treating the cancer. The nano-cluster for treating the cancer prepared by the method can be enriched in tumor tissue parts through the enhanced permeability and retention (EPR) effect, and release the cisplatin and the arsenic trioxide with anti-tumor properties under thepH condition in tumor cells to synergistically inhibit tumor growth, reduce the toxic and side effects on non-lesional sites, and improve the treatment coefficient of tumor sites.

Polyionic type micelle shielding system with electric charge turnover function and preparation method thereof

The invention provides a polyionic type micelle shielding system with reversible charges. The polyionic type micelle shielding system is formed by a compound shown as formula (III) and cis-diamminedichloroplatinum through coordination. According to the polyionic type micelle shielding system with the reversible charges, cis-diamminedichloroplatinum is supported under a coordination action, a support material is good in biocompatibility and solubility, the nano-support is enriched at a tumor tissue part through an EPR (enhanced permeability and retention effect), a shell with a shielding capability is removed under the condition of pH at the tumor tissue part, a positively charged cis-diamminedichloroplatinum supported core is exposed, endocytosis is facilitated by the positively charged core, and after the cis-diamminedichloroplatinum supported core enters a cell, the drug cis-diamminedichloroplatinum with anti-tumor performance is released by the cis-diamminedichloroplatinum supportedcore.

Dual-Emissive Platinum(II) Metallacage with a Sensitive Oxygen Response for Imaging of Hypoxia and Imaging-Guided Chemotherapy

Imaging of hypoxia in vivo helps with accurate cancer diagnosis and evaluation of therapeutic outcomes. A PtII metallacage with oxygen-responsive red phosphorescence and steady fluorescence for in vivo hypoxia imaging and chemotherapy is reported. The therapeutic agent and diagnostic probe were integrated into the metallacage through heteroligation-directed self-assembly. Nanoformulation by encapsulating the metallacage into nanoparticles greatly enhanced its stability the in physiological environment, rendering biomedical applications feasible. Apart from enhanced red phosphorescence upon hypoxia, the ratio between red and blue emissions, which only varies with intracellular oxygen level, provides a more precise standard for hypoxia imaging and detection. Moreover, in vivo explorations demonstrate the promising potential applications of the metallacage-loaded nanoparticles as theranostic agents for tumor hypoxia imaging and chemotherapy.

Folic acid mediated dual-drug-loading targeting polymeric micelle and preparation method and application thereof

The invention discloses a folic acid mediated dual-drug-loading targeting polymeric micelle and a preparation method and application thereof. The polymeric micelle is a nanoparticle formed by that polyglutamic acid grafted with paclitaxel, gemcitabine and folic acid is subjected to electrostatic self-assembly with polylysine. Compared with the prior art, the dual-drug-loading targeting polymeric micelle has advantages that by joint use of paclitaxel and gemcitabine, great antitumor effects can be achieved, the problem of poor water solubility of paclitaxel is solved, efficacy improvement and toxicity reduction are realized by targeting, and probability is provided for cancer targeted low-toxicity treatment.

Redox-Responsive Biomimetic Polymeric Micelle for Simultaneous Anticancer Drug Delivery and Aggregation-Induced Emission Active Imaging

Intelligent polymeric micelles have been developed as potential nanoplatforms for efficient drug delivery and diagnosis. Herein, we successfully prepared redox-sensitive polymeric micelles combined aggregation-induced emission (AIE) imaging as an outstanding anticancer drug carrier system for simultaneous chemotherapy and bioimaging. The amphiphilic copolymer TPE-SS-PLAsp-b-PMPC could self-assemble into spherical micelles, and these biomimetic micelles exhibited great biocompatibility and remarkable ability in antiprotein adsorption, showing great potential for biomedical application. Anticancer drug doxorubicin (DOX) could be encapsulated during the self-assembly process, and these drug-loaded micelles showed intelligent drug release and improved antitumor efficacy due to the quick disassembly in response to high levels of glutathione (GSH) in the environment. Moreover, the intracellular DOX release could be traced through the fluorescent imaging of these AIE micelles. As expected, the in vivo antitumor study exhibited that these DOX-carried micelles showed better antitumor efficacy and less adverse effects than that of free DOX. These results strongly indicated that this smart biomimetic micelle system would be a prominent candidate for chemotherapy and bioimaging.

Synthesis and Characterization of Nitric Oxide-Releasing Platinum(IV) Prodrug and Polymeric Micelle Triggered by Light

Herein, we report the proof of concept of photoresponsive chemotherapeutics comprising nitric oxide-releasing platinum prodrugs and polymeric micelles. Photoactivatable nitric oxide-releasing donors were integrated into the axial positions of a platinum(IV) prodrug, and the photolabile hydrophobic groups were grafted in the block copolymers. The hydrophobic interaction between nitric oxide donors and the photolabile groups allowed for the loading of platinum drugs and nitric oxide-releasing donors in the photolabile polymeric micelles. After cellular uptake of micelles, light irradiation induced the release of nitric oxide, which sensitized the cancer cells. Simultaneously, photolabile hydrophobic groups were cleaved from micelles, and the nitric oxide-releasing donor was altered to be more hydrophilic, resulting in the rapid release of platinum(IV) prodrugs. The strategy of using platinum(IV) prodrugs and nitric oxide led to enhanced anticancer effects.

Novel 3D Neuron Regeneration Scaffolds Based on Synthetic Polypeptide Containing Neuron Cue

Neural tissue engineering has become a potential technology to restore the functionality of damaged neural tissue with the hope to cure the patients with neural disorder and to improve their quality of life. This paper reports the design and synthesis of polypeptides containing neuron stimulate, glutamic acid, for the fabrication of biomimetic 3D scaffold in neural tissue engineering application. The polypeptides are synthesized by efficient chemical reactions. Monomer γ-benzyl glutamate-N-carboxyanhydride undergoes ring-opening polymerization to form poly(γ-benzyl-l-glutamate), then hydrolyzes into poly(γ-benzyl-l-glutamate)-r-poly(glutamic acid) random copolymer. The glutamic acid amount is controlled by hydrolysis time. The obtained polymer molecular weight is in the range of 200 kDa for good quality of fibers. The fibrous 3D scaffolds of polypeptides are fabricated using electrospinning techniques. The scaffolds are biodegradable and biocompatible. The biocompatibility and length of neurite growth are improved with increasing amount of glutamic acid in scaffold. The 3D scaffold fabricated from aligned fibers can guide anisotropic growth of neurite along the fiber and into 3D domain. Furthermore, the length of neurite outgrowth is longer for scaffold made from aligned fibers as compared with that of isotropic fibers. This new polypeptide has potential for the application in the tissue engineering for neural regeneration.

Synthesis of alkyl-modified poly(sodium glutamate)s for preparation of polymer-protein nanoparticles in combination with N,N,N-trimethyl chitosan

The negatively charged, water-soluble, hydrophobically modified poly(sodium glutamate)s containing different amounts of alkyl grafts were synthesized. First, poly(γ-benzyl-L-glutamate) was prepared by ring-opening polymerization of the corresponding N-carboxyanhydride, which was in the next step aminolysed with octylamine. After removal of the remaining benzyl protective groups, the alkyl-modified poly(sodium glutamate)s [P(Glu-oa)] were obtained and, together with the oppositely charged N,N,N-trimethyl chitosan (TMC), used for the preparation of nanoparticles (NPs) of a recombinant granulocyte colony-stimulating factor (GCSF) protein by polyelectrolyte complexation method. It is observed that, beside electrostatic interaction, the hydrophobic grafts on poly(sodium glutamate)s significantly contribute to association efficiency (AE) with GCSF protein. The addition of TMC solution to the dispersion of GCSF/P(Glu-oa) complexes results in formation of much more defined NPs with high AE and final protein loading.