肽和蛋白质的聚乙二醇化：问题与解决方案综述

Peptide and protein PEGylation: a review of problems and solutions.

作者信息

Veronese F M

机构信息

Department of Pharmaceutical Sciences, CNR, Center for Chemical Investigation of Drugs, University of Padova, Italy.

出版信息

Biomaterials. 2001 Mar;22(5):405-17. doi: 10.1016/s0142-9612(00)00193-9.

DOI:10.1016/s0142-9612(00)00193-9

PMID:11214751

Abstract

The paper discusses general problems in using PEG for conjugation to high or low molecular weight molecules. Methods of binding PEG to different functional groups in macromolecules is reported together with their eventual limitations. Problems encountered in conjugation, such as the evaluation of the number of PEG chains bound, the localisation of the site of conjugation in polypeptides and the procedure to direct PEGylation to the desired site in the molecule are discussed. Finally, the paper reports on more specific methods regarding reversible PEGylation, cross-linking reagents with PEG arms, PEG for enzyme solubilization in organic solvent and new polymers as alternative to PEG.

摘要

本文讨论了使用聚乙二醇（PEG）与高分子量或低分子量分子缀合的一般问题。报告了将PEG与大分子中不同官能团结合的方法及其最终局限性。讨论了缀合过程中遇到的问题，例如结合的PEG链数量的评估、多肽中缀合位点的定位以及将聚乙二醇化引导至分子中所需位点的程序。最后，本文报道了关于可逆聚乙二醇化、带有PEG臂的交联试剂、用于在有机溶剂中溶解酶的PEG以及作为PEG替代品的新型聚合物的更具体方法。