| 杨凯睿 高向东 徐晨 童梅 陆小冬.聚乙二醇定点修饰蛋白质药物的技术和临床研究进展[J].现代生物医学进展英文版,2015,15(32):6381-6385. |
| 聚乙二醇定点修饰蛋白质药物的技术和临床研究进展 |
| The Technique and Clinical Development of Site-specific PEGylated ProteinDrugs |
| |
| DOI： |
| 中文关键词: 聚乙二醇定点修饰 定点修饰技术 PEG 修饰药物 临床进展 |
| 英文关键词: Site-specific PEGylation Techinique of site-specific PEGylation PEGylated drugs Clinical development |
| 基金项目:北京市科技计划项目（D08080200290808） |
|
| Hits: 688 |
| Download times: 0 |
| 中文摘要: |
| 聚乙二醇（PEG）定点修饰蛋白药物是针对蛋白特定基团特定位点的修饰，相比于非定点随机修饰的特点是PEG 修饰位点
的单一与确定，避免了修饰异构体的干扰，能较好的保留药物体内外活性；修饰产物组成均一、性质稳定，便于质量控制，降低由
修饰异构体引起的潜在的安全性风险，并很大程度上提高得率，降低成本。已有PEG定点修饰蛋白药物上市，还有部分处于临床
试验阶段。本文综述了PEG 定点修饰蛋白药物的技术研究与临床进展，包括PEG 定点修饰剂、定点修饰方法、PEG 定点修饰的上
市和临床药物及面临的问题，并展望了PEG 修饰技术未来的发展前景。 |
| 英文摘要: |
| Site-specific polyethylene glycol (PEG) modification is the PEGylation of specific site of the protein. Compared with
non-specific PEGylation, the advantages of site-specific PEGylation are the uniqueness of PEGylated site , no interference of modified
isomers, preserved activity in vitro and in vivo; the modified product is homogeneous, stable, and convenient for quality control, and can
reduce side effects of modified isomers, increase production yield and decrease costs. Site-specific PEGylation protein drugs are already
on the market, others are still in clinical trials. This paper reviews the research progress of technique and clinical development of
site-specific PEGylated protein drugs, including typical site-specific PEG modifiers, general methods of site-specific PEGylation,
site-specific PEGylated drugs on the market and in clinical development, and problems faced with by researchers, and looks into the
future development of site-specific PEG modification technique. |
|
View Full Text
View/Add Comment Download reader |
| Close |
