3 years ago

Synthesis, receptor binding studies, optical spectroscopic and in silico structural characterization of morphiceptin analogs with cis-4-amino-L-proline residues

Synthesis, receptor binding studies, optical spectroscopic and in silico structural characterization of morphiceptin analogs with cis-4-amino-L-proline residues
Alicja Kluczyk, Justyna Piekielna-Ciesielska, Anna Janecka, Anna Adamska-Bartłomiejczyk, Csaba Tömböly, Marek Lisowski, Grzegorz Wołczański, Attila Borics, Szabolcs Dvorácskó
Three novel morphiceptin analogs, in which Pro in position 2 and/or 4 was replaced by cis-4-aminoproline connected with the preceding amino acid through the primary amino group, were synthesized. The opioid receptor affinities, functional assay results, enzymatic degradation studies and experimental and in silico structural analysis of such analogs are presented. Copyright © 2017 European Peptide Society and John Wiley & Sons, Ltd. Novel morphiceptin analogs, in which Pro in position 2 and/or 4 was replaced by cis-4-aminoproline connected with the preceding amino acid through the primary amine, were synthesized. Analog with two cis-4-aminoproline residues, exhibited a three orders of magnitude increase of mu opioid receptor affinity. Significant increase of flexibility could be responsible for the much better structural adaptation of this analog to the shape of the binding cavity, explaining extraordinary mu affinity.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/psc.3050

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