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EnglishIn the last few years we discovered and investigated novel cyclic opioid peptides, c[Tyr-Xaa-D-Trp- Phe-Yaa], based on the sequence of EM-1. These peptides, deprived of a protonable amino group, bind and activate the MOR receptor mainly through the side chains of the amino acids 2 and 3, as revealed by molecular docking analysis. As a consequence, we synthesized and tested short di- and tri-peptides containing the sequence D-Trp- Phe, aiming to determine the minimal requisites necessary for the pharmacological effect. This study lead to the new linear peptides Ac-D-Trp-PheNH2 and Ac-D-Trp-Phe-GlyNH2, which revealed a good affinity for MOR, and agonist efficacy in vivo. Substitution of D-Trp with other amino acids gave inactive compounds or moderate antagonism. Conformational analysis and docking suggested that the short peptides adopt a bioactive conformation characterized by a beta-turn.
| Titolo: | Ac-D-Trp-PheNH2 AND Ac-D-Trp-Phe-GlyNH2 - A NEW CLASS OF UNUSUAL OPIOID PEPTIDES | |
| Autore/i: | GENTILUCCI, LUCA; DE MARCO, ROSSELLA; TOLOMELLI, ALESSANDRA; SPAMPINATO, SANTI MARIO; BEDINI, ANDREA; R. Artali | |
| Autore/i Unibo: | ||
| Anno: | 2010 | |
| Titolo del libro: | INRC 2010 - Abstracts Book | |
| Pagina iniziale: | 79 | |
| Pagina finale: | 79 | |
| Abstract: | In the last few years we discovered and investigated novel cyclic opioid peptides, c[Tyr-Xaa-D-Trp- Phe-Yaa], based on the sequence of EM-1. These peptides, deprived of a protonable amino group, bind and activate the MOR receptor mainly through the side chains of the amino acids 2 and 3, as revealed by molecular docking analysis. As a consequence, we synthesized and tested short di- and tri-peptides containing the sequence D-Trp- Phe, aiming to determine the minimal requisites necessary for the pharmacological effect. This study lead to the new linear peptides Ac-D-Trp-PheNH2 and Ac-D-Trp-Phe-GlyNH2, which revealed a good affinity for MOR, and agonist efficacy in vivo. Substitution of D-Trp with other amino acids gave inactive compounds or moderate antagonism. Conformational analysis and docking suggested that the short peptides adopt a bioactive conformation characterized by a beta-turn. | |
| Data prodotto definitivo in UGOV: | 21-feb-2011 | |
| Appare nelle tipologie: | 4.02 Riassunto (Abstract) |
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