Abstract
Despite of the recent advances in the structural investigation of complex molecules, the comprehension of the 3D features responsible for the interaction between opioid peptides and μ- opioid receptors still remains an elusive task. This has to be attributed to the intrinsic nature of opioid peptides, which can assume a number of different conformations of similar energy, and to the flexibility of the receptorial cavity, which can modify its inner shape to host different ligands. Due to this inherent mobility of the ligand-receptor system, massive efforts devoted to the definition of a rigid bioactive conformation to be used as a template for the design of new pharmacologically active compounds might be overstressed. The future goal might be the design of peptide or nonpeptide ligands capable of maximizing specific hydrophobic interactions. This review covers the recent opinions emerged on the nature of the ligand-receptor interaction, and the development of suitable models for the determination of the bioactive conformation of peptide ligands active towards m-opioid receptors.
Keywords: Opioid peptides, endomorphins, bioactive conformation, antinociception
Current Topics in Medicinal Chemistry
Title: Recent Advances in the Investigation of the Bioactive Conformation of Peptides Active at the μ-opioid Receptor. Conformational Analysis of Endomorphins
Volume: 4 Issue: 1
Author(s): Luca Gentilucci and Alessandra Tolomelli
Affiliation:
Keywords: Opioid peptides, endomorphins, bioactive conformation, antinociception
Abstract: Despite of the recent advances in the structural investigation of complex molecules, the comprehension of the 3D features responsible for the interaction between opioid peptides and μ- opioid receptors still remains an elusive task. This has to be attributed to the intrinsic nature of opioid peptides, which can assume a number of different conformations of similar energy, and to the flexibility of the receptorial cavity, which can modify its inner shape to host different ligands. Due to this inherent mobility of the ligand-receptor system, massive efforts devoted to the definition of a rigid bioactive conformation to be used as a template for the design of new pharmacologically active compounds might be overstressed. The future goal might be the design of peptide or nonpeptide ligands capable of maximizing specific hydrophobic interactions. This review covers the recent opinions emerged on the nature of the ligand-receptor interaction, and the development of suitable models for the determination of the bioactive conformation of peptide ligands active towards m-opioid receptors.
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Gentilucci Luca and Tolomelli Alessandra, Recent Advances in the Investigation of the Bioactive Conformation of Peptides Active at the μ-opioid Receptor. Conformational Analysis of Endomorphins, Current Topics in Medicinal Chemistry 2004; 4 (1) . https://dx.doi.org/10.2174/1568026043451627
DOI https://dx.doi.org/10.2174/1568026043451627 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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