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

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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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Keywords: Dimerization; Endomorphin-2; Opioid receptor; Structure-activity relationships; analogue; balanced agonist

Document Type: Research Article

Publication date: March 1, 2008

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  • Protein & Peptide Letters publishes short papers in all important aspects of protein and peptide research, including structural studies, recombinant expression, function, synthesis, enzymology, immunology, molecular modeling, drug design etc. Manuscripts must have a significant element of novelty, timeliness and urgency that merit rapid publication. Reports of crystallisation, and preliminary structure determinations of biologically important proteins are acceptable. Purely theoretical papers are also acceptable provided they provide new insight into the principles of protein/peptide structure and function.
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