Issue 18, 2015

Novel reactive PEG for amino group conjugation

Abstract

Activated mPEG carbonates are important reagents that have been widely used for the PEGylation of several peptides and proteins by means of stable urethane linkages. In fact, mPEG-N-hydroxysuccinimidyl carbonate and mPEG-p-nitrophenyl carbonate are among the most used reagents in PEGylation technology. However, the synthesis and storage of these reagents are not always easy to resolve. With the aim of surpassing some of the drawbacks associated with the use of activated mPEG-carbonates we have prepared and evaluated a new mPEG-carbonylimidazolium iodide, which can be used for the conjugation of the NH2 group by means of urethane linkages, as an interesting alternative to the known reagents. It is noteworthy that the novel reagent is prepared by a simple two-step procedure under mild experimental conditions. Moreover, we performed a detailed study of the conjugation reaction of interferon-α2b with the carbonylimidazolium derivative, and evaluated the conjugate in in vitro and in vivo studies.

Graphical abstract: Novel reactive PEG for amino group conjugation

Supplementary files

Article information

Article type
Paper
Submitted
25 Nov 2014
Accepted
21 Jan 2015
First published
21 Jan 2015

RSC Adv., 2015,5, 14002-14009

Author version available

Novel reactive PEG for amino group conjugation

M. González, N. A. Ceaglio, M. de los Milagros Bürgi, M. Etcheverrigaray, R. B. Kratje and S. E. Vaillard, RSC Adv., 2015, 5, 14002 DOI: 10.1039/C5RA00758E

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements