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Protein & Peptide Letters

Editor-in-Chief

ISSN (Print): 0929-8665
ISSN (Online): 1875-5305

Structure-Activity Relationships of the Dimeric Analogues of Endomorphin-2 with Different Lengths of Spacers

Author(s): Yuan-Ming Qi, Yan-Feng Gao, Ming-Xia Zhai, Wei-Xia Liu, Xin Liu, Ye Yuan and Rui Wang

Volume 15, Issue 3, 2008

Page: [275 - 279] Pages: 5

DOI: 10.2174/092986608783744199

Price: $65

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


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