Abstract
In the present study, seven novel dimeric analogues of endomorphin-2 with longer spacers were designed and synthesized. Through dimerization, their affinity for δ-opioid receptor was mostly increased, especially the δ-opioid receptor preferred dimeric analogue, DEM12. The results were confirmed by the in vitro bioassay. The structure-activity relationships were also discussed.
Keywords: Endomorphin-2, Dimerization, analogue, Structure-activity relationships, Opioid receptor, balanced agonist
Protein & Peptide Letters
Title: Structure-Activity Relationships of the Dimeric Analogues of Endomorphin-2 with Different Lengths of Spacers
Volume: 15 Issue: 3
Author(s): Yuan-Ming Qi, Yan-Feng Gao, Ming-Xia Zhai, Wei-Xia Liu, Xin Liu, Ye Yuan and Rui Wang
Affiliation:
Keywords: Endomorphin-2, Dimerization, analogue, Structure-activity relationships, Opioid receptor, balanced agonist
Abstract: In the present study, seven novel dimeric analogues of endomorphin-2 with longer spacers were designed and synthesized. Through dimerization, their affinity for δ-opioid receptor was mostly increased, especially the δ-opioid receptor preferred dimeric analogue, DEM12. The results were confirmed by the in vitro bioassay. The structure-activity relationships were also discussed.
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Cite this article as:
Qi Yuan-Ming, Gao Yan-Feng, Zhai Ming-Xia, Liu Wei-Xia, Liu Xin, Yuan Ye and Wang Rui, Structure-Activity Relationships of the Dimeric Analogues of Endomorphin-2 with Different Lengths of Spacers, Protein & Peptide Letters 2008; 15 (3) . https://dx.doi.org/10.2174/092986608783744199
DOI https://dx.doi.org/10.2174/092986608783744199 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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