Bioconjugation in pharmaceutical chemistry

Veronese, Francesco M.; Morpurgo, Margherita

doi:10.1016/s0014-827x(99)00066-x

Cited by 154 publications

(86 citation statements)

References 108 publications

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“…The solution was stirred for 1 h at room temperature and further on for 16 h at 48C, and applied to a gel filtration column Fractogel EMD BioSEC (S) (2.6 Â 60 cm 2 ), equilibrated in 20 mM sodium phosphate buffer, pH 7.0, containing 100 mM NaCl. The fractions containing the polymer-enzyme conjugate were pooled and kept at 48C.…”

Section: Preparation Of Catalase-dextran Conjugatementioning

confidence: 99%

“…2 In special, poly(ethylene glycol) (PEG) has been widely used for site-directed modification of protein drugs, and there are many PEG-based protein conjugates in the market with increased circulatory half-life. 3 However, PEG is a non biodegradable macromolecule which is slowly cleared from the human body, and the occurrence of anaphylactic reactions and a severe bronchospasm have been reported for PEGmodified therapeutic enzymes.…”

Section: Introductionmentioning

confidence: 99%

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Improved pharmacokinetics and stability properties of catalase by chemical glycosidation with end‐group activated dextran

Villalonga

Valdivia

Pérez

et al. 2006

J of Applied Polymer Sci

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Section: Preparation Of Catalase-dextran Conjugatementioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Improved pharmacokinetics and stability properties of catalase by chemical glycosidation with end‐group activated dextran

Villalonga

Valdivia

Pérez

et al. 2006

J of Applied Polymer Sci

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“…Modification of the surface of enzymes, using synthetic biocompatible polymers such as poly(ethylene glycol) (PEG) of various molecular masses (Fortier, 1994;Veronese and Morpurgo, 1999), is a well established tool to increase the functional stability of the proteins and to diminish their blood clearance as well as their immunogenicity.…”

Section: Introductionmentioning

confidence: 99%

Polyketone polymer: A new support for direct enzyme immobilization

Agostinelli

Belli

Tempera

et al. 2007

Journal of Biotechnology

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Polyketone polymer [ CO CH 2 CH 2 ] n , obtained by copolymerization of ethene and carbon monoxide, is utilized for immobilization of three different enzymes, one peroxidase from horseradish (HRP) and two amine oxidases, from bovine serum (BSAO) and lentil seedlings (LSAO). The easy immobilization procedure is carried out in diluted buffer, at pH 7.0 and 3 • C, gently mixing the proteins with the polymer. No bifunctional reagents and spacer arms are required for the immobilization, which occurs exclusively via a large number of hydrogen bonds between the carbonyl groups of the polymer and the NH groups of the polypeptidic chain. Experiments demonstrate a high linking capacity of polymer for BSAO and an extraordinary strong linkage for LSAO. Moreover, activity measurements demonstrate that immobilized LSAO totally retains the catalytic characteristics of the free enzyme, where only a limited increase of K M value is observed. Finally, the HRP-activated polymer is successfully used as active packed bed of an enzymatic reactor for continuous flow conversion and flow injection analysis of hydrogen peroxide containing solutions.

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“…Polyaminoacid polymers with various side functional groups suitable for modification and conjugation with active molecules are available (3). Among polyaminoacids, polyaspartamide derivatives have been of special interest due to their excellent solubility, bioavailability, biocompatibility and favorable reactivity (1). Polyaspartamide conjugates with numerous drugs have been reported by our (4)(5)(6) and other research groups (see, for example, refs.…”

mentioning

confidence: 99%

Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer

Končić¹,

Zorc²,

Novak³

2011

Acta Pharmaceutica

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Polymer-drug conjugates are macromolecular drug carrier systems with active agents attached as side substituents to a polymer backbone using an appropriate spacer. They could be an effective way to prolong drug activity, minimize unfavorable side effects and toxicity, decrease the required dose and increase the solubility of drugs (1). In addition, polymer-drug conjugates have the ability to overpass some mechanisms of drug resistance and the potential to elicit immunostimulatory effects. They can also alter the body distribution of drugs and ensure adequate drug delivery to target cells or tissues. This is Two hydrosoluble conjugates of 17b-estradiol (ED) and estradiol-17b-valerate (EV) with polyaspartamide polymer were prepared and characterized. ED and EV were first chemically modified and bound to poly[a,b-(N-2-hydroxyethyl-DL-aspartamide)]-poly[a,b-(N-2-aminoethyl-DL-aspartamide)] (PAHA), a hydrosoluble polyaspartamide--type copolymer bearing both hydroxyl and amino groups. ED was first converted to 17-hemisuccinate (EDS) and then bound to PAHA. In the resulting conjugate PAHA-EDS, the estradiol moiety was linked to the polymer through a 2-aminoethylhemisuccinamide spacer. On the other hand, EV was first converted to estradiol-17b-valerate-3--(benzotriazole-1-carboxylate), which readily reacted with amino groups in PAHA affording the polymer-drug conjugate PAHA-EV. In the prepared conjugate PAHA-EV, the estradiol moiety was covalently bound to the polyaspartamide backbone by carbamate linkage, through an ethylenediamine spacer. The polymer-drug conjugates were designed and prepared with the aim to increase water--solubility, bioavailability and to improve drug delivery of the lipophilic estrogen hormone.

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Bioconjugation in pharmaceutical chemistry

Cited by 154 publications

References 108 publications

Improved pharmacokinetics and stability properties of catalase by chemical glycosidation with end‐group activated dextran

Improved pharmacokinetics and stability properties of catalase by chemical glycosidation with end‐group activated dextran

Polyketone polymer: A new support for direct enzyme immobilization

Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer

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