Jump to main content
Jump to site search

Issue 53, 2015
Previous Article Next Article

Synthesis of 4-aminobenzoic acid esters of polyethylene glycol and their use for pegylation of therapeutic proteins

Author affiliations

Abstract

As the majority of reagents commonly used for protein pegylation have certain disadvantages concerning their reactivity, stability, convenience and selectivity of pegylation reaction, etc., the search for new pegylation reagents is of current interest. In the present paper, 4-aminobenzoic acid esters of polyethylene glycol are considered as promising pegylation reagents for chemical modification of molecules of biologically active proteins to prepare their conjugates characterized by improved therapeutic properties. These reagents are highly reactive and stable and make it possible to perform histidine- and tyrosine-targeted pegylation of protein chains. The convenient technique for the synthesis of 4-aminobenzoic acid esters of polyethylene glycol was optimized to prepare these pegylation reagents with actual quantitative loading of the polymer with the functional group (the residue of 4-aminobenzoic acid). The efficiency of the synthesized compounds was shown in the pegylation of such proteins as interferon α-2b and erythropoietin β and it was found that the activity of the prepared interferon α-2b conjugate is comparable with those of its commercial analogs such as Pegintron® and Pegasys®.

Graphical abstract: Synthesis of 4-aminobenzoic acid esters of polyethylene glycol and their use for pegylation of therapeutic proteins

Back to tab navigation

Supplementary files

Article information


Submitted
20 Mar 2015
Accepted
06 May 2015
First published
06 May 2015

RSC Adv., 2015,5, 42903-42909
Article type
Paper
Author version available

Synthesis of 4-aminobenzoic acid esters of polyethylene glycol and their use for pegylation of therapeutic proteins

D. V. Lonshakov, S. V. Sheremet'ev, E. M. Belosludtseva, S. A. Korovkin, A. V. Semchenko and A. V. Katlinskij, RSC Adv., 2015, 5, 42903
DOI: 10.1039/C5RA04950D

Social activity

Search articles by author

Spotlight

Advertisements