Search results for "Bioconjugation"
showing 10 items of 30 documents
Synthesis and noncovalent protein conjugation of linear-hyperbranched PEG-poly(glycerol) alpha,omega(n)-telechelics.
2009
Linear-hyperbranched, heterobifunctional alpha,omega(n) telechelic block copolymers consisting of a linear poly(ethylene glycol) (PEG) chain and a hyperbranched polyglycerol (PG) block have been prepared in five steps, using a protected amino-functional initiator. The polyfunctionality omega(n) (OH groups) can be adjusted by the degree of polymerization (DP(n)) of the polyglycerol block. Subsequent introduction of a single biotin unit by amidation in alpha-position permitted noncovalent bioconjugation with avidin.
SYNTHESIS, PHYSICO-CHEMICAL AND BIOLOGICAL CHARACTERIZATION OF A PACLITAXEL MACROMOLECULAR PRODRUG
2004
Paclitaxel was attached to poly(hydroxyethylaspartamide) via a succinic spacer arm by a two-step protocol: (1) synthesis of 2'-O-succinyl-paclitaxel; (2) synthesis of PHEA-2'-O-succinyl-paclitaxel. The 2'-O-succinyl-paclitaxel derivative and the macromolecular conjugate were characterized by UV, IR, NMR and mass spectrometry analysis. The reaction yields were over 95% and the purity of products over 98%. Paclitaxel release and degradation from 2'-O-succinyl-paclitaxel occurred at a faster rate at pH 5.5 than 7.4. After 30 h of incubation at pH 5.5 and 7.4 the released free paclitaxel was about 40 and 20%, respectively. In plasma both drug release and degradation were found to occur at a hig…
Stacking as a key property for creating nanoparticles with tunable shape: The case of squalenoyl-doxorubicin
2019
The development of elongated nanoparticles for drug delivery is of growing interest in recent years, due to longer blood circulation and improved efficacy compared to spherical counterparts. Squalenoyl-doxorubicin (SQ-Dox) conjugate was previously shown to form elongated nanoparticles with improved therapeutic efficacy and decreased toxicity compared to free doxorubicin. By using experimental and computational techniques, we demonstrate here that the specific physical properties of SQ-Dox, which include stacking and electrostatic interactions of doxorubicin as well as hydrophobic interactions of squalene, are involved in the formation of nanoassemblies with diverse elongated structures. We …
Synthesis of site-heterologous haptens for high-affinity anti-pyraclostrobin antibody generation.
2011
The design and synthesis of functional chemical derivatives of small organic molecules is usually a key step for the intricate production of a variety of bioconjugates. In this respect, the derivatization site at which the spacer arm is introduced in immunizing conjugates constitutes a highly critical parameter for the generation of high-affinity and selective antibodies. However, due to the usual complexity of the required synthetic procedures, the appropriate comparison of alternative tethering positions has often been neglected. In the present study, meticulous strategies were followed to prepare synthetic derivatives of pyraclostrobin with the same linkers located at diverse rationally-…
Structure and biological evaluation of amino-functionalized PVP nanogels for fast cellular internalization
2013
Abstract Aminopropyl methacrylamide chloride-graft-poly(N-vinyl pyrrolidone) nanogels (NGs) were designed to exploit the favorable properties of poly(N-vinyl pyrrolidone) (PVP), such as its high affinity to water and complexation ability of ions, molecules and macromolecules, with the availability of primary amino groups for bioconjugation reactions. A thorough structural characterization of the nanoscalar networks was performed via 1 H NMR and solid state 13 C NMR spectroscopies, while solid state NMR relaxation time measurements completed the NGs description in terms of polymer network density. Information on the hydrodynamic size and surface charge densities were sought via dynamic light…
Biomolecular conjugation inside synthetic polymer nanopores via glycoprotein-lectin interactions
2011
We demonstrate the supramolecular bioconjugation of concanavalin A (Con A) protein with glycoenzyme horseradish peroxidase (HRP) inside single nanopores, fabricated in heavy ion tracked polymer membranes. Firstly, the HRP-enzyme was covalently immobilized on the inner wall of the pores using carbodiimide coupling chemistry. The immobilized HRP-enzyme molecules bear sugar (mannose) groups available for the binding of Con A protein. Secondly, the bioconjugation of Con A on the pore wall was achieved through its biospecific interactions with the mannose residues of the HRP enzyme. The immobilization of biomolecules inside the nanopore leads to the reduction of the available area for ionic tran…
Silicatein conjugation inside nanoconfined geometries through immobilized NTA–Ni(ii) chelates
2013
The chemical modification and bioconjugation processes inside confined geometries by His-tagged silicatein promote sensitive changes in the polarity and surface charge density that mainly contribute to the ionic current rectification properties of the single conical nanopores.
Minimalism in radiation synthesis of biomedical functional nanogels.
2012
A scalable, single-step, synthetic approach for the manufacture of biocompatible, functionalized micro- and nanogels is presented. In particular, poly(N-vinyl pyrrolidone)-grafted-(aminopropyl)methacrylamide microgels and nanogels were generated through e-beam irradiation of PVP aqueous solutions in the presence of a primary amino-group-carrying monomer. Particles with different hydrodynamic diameters and surface charge densities were obtained at the variance of the irradiation conditions. Chemical structure was investigated by different spectroscopic techniques. Fluorescent variants were generated through fluorescein isothiocyanate attachment to the primary amino groups grafted to PVP, to …
New site-specific bioconjugation strategies and their application to the development of molecular imaging agents for cancer diagnostic
2018
The preparation of targeted imaging agents suitable for cancer diagnostic involves the coupling of an imaging probe to a vector, generally a protein, able to specifically target cancerous tissues. Unfortunately, this bioconjugation step is often problematic. Indeed, proteins present a large variety of reactive functions that can potentially interfere with the coupling reaction. The purpose of this work is the design of innovative selective bioconjugation strategies that can facilitate the synthesis of molecular imaging agents.Our research led to the development of a simple and efficient approach allowing the modification of a protein with a fluorophore by using a site-specific bioconjugatio…
Multifunctional platforms for cancer theranosis
2018
The objective of this thesis was to develop multifunctional tools for cancer theranosis, particularly based on nanotechnology. The work is based on the premise of monomolecular multimodal platform that aims to create the building blocks that can be used for the synthesis of functionalized nanoparticles, bioconjugates or targeted small molecular imaging probes.The initial work focused on the synthesis of the chelator based silane precursors. These novel precursors were employed for the functionalization of AGuIX nanoparticles and have also been implicated in a one pot AGuIX synthesis. Radiolabelling of these nanoparticles was performed with the aim to evaluate the stability of these nanopart…