Disulfide bridge based conjugation of peptides to RAFT polymers

作者：McDowall Lyndal; Stenzel Martina H^*

来源：Polymer Chemistry, 2014, 5(5): 1772-1781.

DOI：10.1039/c3py01412f

The reaction between bisulfones and the disulfide bridge of peptides or proteins allows the efficient bioconjugation without the loss of biological activity, which is often based on the three-dimensional structure of the biomolecule. This concept has been successfully applied using low molecular weight model compounds and PEG. In this article, RAFT polymers were postmodified to introduce bisulfone end-functionalities. This general approach has been tested here using poly(N-vinylpyrrolidone) PVP, which was prepared via RAFT polymerization. RAFT endgroup removal, followed by the reaction with divinyl sulfone and the bisulfone linker led to a disulfide reactive polymer. NMR studies, MALDI-TOF MSMS and SDS-PAGE confirm the successful reaction between somatostatin, a cyclic hormone peptide and the end-functionalized PVP. The RAFT process as a source to potential polymers widens the scope of this bioconjugation technique to a large array of potential structures.

• 出版日期2014-3-7