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

页码：275 / 279

页数：5

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