UCL School of Pharmacy, 29-39 Brunswick Square, London, WC1N 1AX, UK.
Future Med Chem. 2014;6(16):1829-46. doi: 10.4155/fmc.14.125.
PEGylation is the covalent conjugation of PEG to therapeutic molecules. Protein PEGylation is a clinically proven approach for extending the circulation half-life and reducing the immunogenicity of protein therapeutics. Most clinically used PEGylated proteins are heterogeneous mixtures of PEG positional isomers conjugated to different residues on the protein main chain. Current research is focused to reduce product heterogeneity and to preserve bioactivity. Recent advances and possible future directions in PEGylation are described in this review. So far protein PEGylation has yielded more than 10 marketed products and in view of the lack of equally successful alternatives to extend the circulation half-life of proteins, PEGylation will still play a major role in drug delivery for many years to come.
聚乙二醇化是指将 PEG 通过共价键连接到治疗分子上。蛋白质聚乙二醇化是一种经过临床验证的方法，可延长蛋白质治疗药物的循环半衰期并降低其免疫原性。大多数临床应用的聚乙二醇化蛋白质是聚乙二醇位置异构体与蛋白质主链上不同残基连接的不均一混合物。目前的研究重点是降低产品的不均一性并保持生物活性。本文综述了聚乙二醇化的最新进展和可能的未来方向。到目前为止，已有超过 10 种上市的聚乙二醇化蛋白质产品，鉴于缺乏同样成功的替代方法来延长蛋白质的循环半衰期，聚乙二醇化在未来许多年内仍将在药物输送中发挥重要作用。
