Investigation on PEGylation strategy of recombinant human interleukin-1 receptor antagonist

CORC > 过程工程研究所 > 中国科学院过程工程研究所 > 研究所（批量导入）

	Investigation on PEGylation strategy of recombinant human interleukin-1 receptor antagonist
	Yu, Pengzhan ; Zheng, Chunyang ; Chen, Jing ; Zhang, Guifeng ; Liu, Yongdong ; Suo, Xiaoyan ; Zhang, Guicai ; Su, Zhiguo
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2007-08-15
卷号	15 期号:16 页码:5396-5405
关键词	interleukin-1 receptor antagonist PEGylation binding activities to the receptors
ISSN号	0968-0896
其他题名	Bioorg. Med. Chem.
中文摘要	Although PEGylation is a potential approach to prolong the half-lives and reduce the dosing frequency of therapeutic proteins, conjugation behaviors of polymer have pivotal effects on the remaining bioactivities of the derivatives. In this study, the PEGylation strategy of recombinant human interleukin-1 receptor antagonist was investigated. The random conjugation of polyethylene glycol to amino groups on the protein resulted in a severe loss of activity and only retained 9.8% of the activity. In contrast, the PEGylation at the thiol groups had moderate effects on the bioactivity of protein and 40% of activity was conserved. The results suggested that the thiol-target PEGylation was more beneficial for IL-1ra. (c) 2007 Elsevier Ltd. All rights reserved.
英文摘要	Although PEGylation is a potential approach to prolong the half-lives and reduce the dosing frequency of therapeutic proteins, conjugation behaviors of polymer have pivotal effects on the remaining bioactivities of the derivatives. In this study, the PEGylation strategy of recombinant human interleukin-1 receptor antagonist was investigated. The random conjugation of polyethylene glycol to amino groups on the protein resulted in a severe loss of activity and only retained 9.8% of the activity. In contrast, the PEGylation at the thiol groups had moderate effects on the bioactivity of protein and 40% of activity was conserved. The results suggested that the thiol-target PEGylation was more beneficial for IL-1ra. (c) 2007 Elsevier Ltd. All rights reserved.
WOS标题词	Science & Technology ; Life Sciences & Biomedicine ; Physical Sciences
类目[WOS]	Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]	SITE-SPECIFIC MUTAGENESIS ; CHRONIC HEPATITIS-C ; POLYETHYLENE-GLYCOL ; DRUG-DELIVERY ; RHEUMATOID-ARTHRITIS ; PROTEIN MODIFICATION ; DOUBLE-BLIND ; ASSAY ; PHARMACEUTICALS ; IDENTIFICATION
收录类别	SCI
原文出处	://WOS:000248172700003
语种	英语
WOS记录号	WOS:000248172700003
公开日期	2013-10-15
内容类型	期刊论文
版本	出版稿
源URL	[http://ir.ipe.ac.cn/handle/122111/3499]
专题	过程工程研究所_研究所（批量导入）
作者单位	1.Chinese Acad Sci, Inst Proc Engn, Natl Key Lab Biochem Engn, Beijing 100080, Peoples R China 2.Chinese Acad Sci, Grad Univ, Beijing 100039, Peoples R China 3.Beijing Baiao Pharmaceut Co Ltd, Beijing 102200, Peoples R China
推荐引用方式 GB/T 7714	Yu, Pengzhan,Zheng, Chunyang,Chen, Jing,et al. Investigation on PEGylation strategy of recombinant human interleukin-1 receptor antagonist[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2007,15(16):5396-5405.
APA	Yu, Pengzhan.,Zheng, Chunyang.,Chen, Jing.,Zhang, Guifeng.,Liu, Yongdong.,...&Su, Zhiguo.(2007).Investigation on PEGylation strategy of recombinant human interleukin-1 receptor antagonist.BIOORGANIC & MEDICINAL CHEMISTRY,15(16),5396-5405.
MLA	Yu, Pengzhan,et al."Investigation on PEGylation strategy of recombinant human interleukin-1 receptor antagonist".BIOORGANIC & MEDICINAL CHEMISTRY 15.16(2007):5396-5405.