Topological Exploration of Cyclic Endomorphin-1 Analogues, Structurally Defined Models for Investigating the Bioactive Conformation of MOR Agonists

Title: Topological Exploration of Cyclic Endomorphin-1 Analogues, Structurally Defined Models for Investigating the Bioactive Conformation of MOR Agonists

Volume: 14 Issue: 1

Author(s): Luca Gentilucci, Alessandra Tolomelli and Federico Squassabia

Affiliation:

Keywords: Cyclic endomorphins, bioactive conformation, agonism, MORs, lipophilic peptides

Abstract: Although there have been several reports on the conformational analysis of endomorphin-1 (YPWF-NH2) and related MOR (μ-opioid receptor) agonists, a definitive, convincing model of the biologically active structure is not yet available. We recently reported the synthesis and pharmacological characterization of the atypical endomorphin-analogue agonist c[YpwFG]. In this paper we discuss the conformational analysis of c[YpwFG] in comparison to its epimers, for investigating the topological features responsible for ligand recognition and receptor activation, and the role of the different pharmacophores.

Cite this article as:

Gentilucci Luca, Tolomelli Alessandra and Squassabia Federico, Topological Exploration of Cyclic Endomorphin-1 Analogues, Structurally Defined Models for Investigating the Bioactive Conformation of MOR Agonists, Protein & Peptide Letters 2007; 14 (1) . https://dx.doi.org/10.2174/092986607779117218

DOI https://dx.doi.org/10.2174/092986607779117218	Print ISSN 0929-8665
Publisher Name Bentham Science Publisher	Online ISSN 1875-5305