Structure-activity relationships of the dimeric analogues of endomorphin-2 with different lengths of spacers

被引:0
|
作者
Gao, Yan-Feng [1 ]
Zhai, Ming-Xia [1 ]
Liu, Wei-Xia [2 ]
Liu, Xin [2 ]
Yuan, Ye [2 ]
Qi, Yuan-Ming [1 ]
Wang, Rui [2 ]
机构
[1] Zhengzhou Univ, Dept Bioengn, Zhengzhou 450001, Peoples R China
[2] Lanzhou Univ, Sch Life Sci, Inst Biochem & Mol Biol, Lanzhou 730000, Peoples R China
来源
PROTEIN AND PEPTIDE LETTERS | 2008年 / 15卷 / 03期
关键词
endomorphin-2; dimerization; analogue; structure-activity relationships; opioid receptor; balanced agonist;
D O I
暂无
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
In the present study, seven novel dimeric analogues of endomorphin-2 with longer spacers were designed and synthesized. Through dimerization, their affinity for opioid receptor was mostly increased, especially the delta-opioid receptor preferred dimeric analogue, DEM12. The results were confirmed by the in vitro bioassay. The structure-activity relationships were also discussed.
引用
收藏
页码:275 / 279
页数:5
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