Selective conjugation of poly(2-ethyl 2-oxazoline) to granulocyte colony stimulating factor.

作者: Anna Mero , Zhihao Fang , Gianfranco Pasut , Francesco M. Veronese , Tacey X. Viegas

DOI: 10.1016/J.JCONREL.2012.02.025

关键词:

摘要: Poly(2-ethyl 2-oxazoline) (PEOZ) is a water-soluble, stable and biocompatible polymer that was prepared in linear form for the conjugation of protein biomolecules. Polymers molecular weights ranging from 5 to 20 kDa, with an aldehyde or amine functional terminal group, were synthesized narrow polydispersities. To assess suitability therapeutic application, granulocyte colony stimulating factor (G-CSF) used as model PEOZ conjugation. Two coupling strategies employed, namely chemical N-terminal reductive amination enzymatic transglutaminase (TGase) mediated glutamine The secondary structure protein, measured by circular dichroism, maintained upon PEOZylation stability conjugates toward aggregation at 37 °C improved compared G-CSF. potency PEOZ-G-CSF mono-conjugates tested vitro cell proliferation assays vivo studying effects on white blood neutrophil count increases normal rats. results have shown suitable both methods G-CSF retained high biological activity, vivo.

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