Topological Exploration of Cyclic Endomorphin-1 Analogues, Structurally Defined Models for Investigating the Bioactive Conformation of MOR Agonists
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.
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Document Type: Research Article
Affiliations: Dipartimento di Chimica “G. Ciamician”, via Selmi 2, Università degli Studi di Bologna, 40126 - Bologna, Italy.
Publication date: 2007-01-01
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