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Special Issue "Neuropeptides Involved in Pain Control"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (15 October 2019).

Special Issue Editors

Prof. Dr. Adriano Mollica
Website
Guest Editor
University "G. d'Annunzio" of Chieti-Pescara, Chieti, Italy
Interests: opioid peptides; cannabinoids; amino acids,nutraceuticals, bioactive compounds
Dr. Azzurra Stefanucci
Website
Guest Editor
University of G. d'Annunzio Chieti and Pescara, Department of Pharmacy, Chieti, Italy
Interests: synthesis, characterization, extraction, NMR, purification, nutraceutic

Special Issue Information

Dear Colleagues,

Neuropeptides are well-defined chemical molecules, produced and released by the central nervous system and peripheral. They are involved in the transmission, modulation, and perception of physiological, neuropathic, and inflammatory pain. The development of novel nonpeptide agonists/antagonists, molecular cloning techniques, and transgenic animal models helps to define their functions in the nociceptive cascade, revealing a complex pattern of molecular mechanisms. Often, they are co-localized with neurotransmitters at the same nerve ending, blocking or enhancing their effects. For example, the calcitonin-gene-related peptide (CGRP) and neuropeptide tyrosine (NPY) are expressed and released from non-neuronal cells, acting via the same receptors as their neuronal counterparts. Peptides are endowed with a pleiotropic function, which is responsible for their plasticity under normal and experimental conditions, and redundancy, which may account for the poor performance of individual neuropeptide inhibitors in clinical trials. Accordingly, this Special Issue is focused on the design, synthesis, and biological evaluation of novel neuropeptides with the hope to replace or, at least, complement the use of opiate drugs, leading to increased efficacy and reduced adverse effects.

Prof. Adriano Mollica
Dr. Azzurra Stefanucci
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2000 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Neuropeptides
  • Pain
  • Opioid system
  • Cannabinoids
  • Peptide synthesis
  • Peptidomimetics
  • Peptide application
  • Peptide cell-targeting
  • Peptide design

Published Papers (1 paper)

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Research

Open AccessArticle
Discovery of Novel µ-Opioid Receptor Inverse Agonist from a Combinatorial Library of Tetrapeptides through Structure-Based Virtual Screening
Molecules 2019, 24(21), 3872; https://doi.org/10.3390/molecules24213872 - 27 Oct 2019
Cited by 7
Abstract
Morphine, oxycodone, fentanyl, and other µ-opioid receptors (MOR) agonists have been used for decades in antinociceptive therapies. However, these drugs are associated with numerous side effects, such as euphoria, addiction, respiratory depression, and adverse gastrointestinal reactions, thus, circumventing these drawbacks is of extensive [...] Read more.
Morphine, oxycodone, fentanyl, and other µ-opioid receptors (MOR) agonists have been used for decades in antinociceptive therapies. However, these drugs are associated with numerous side effects, such as euphoria, addiction, respiratory depression, and adverse gastrointestinal reactions, thus, circumventing these drawbacks is of extensive importance. With the aim of identifying novel peptide ligands endowed with MOR inhibitory activity, we developed a virtual screening protocol, including receptor-based pharmacophore screening, docking studies, and molecular dynamics simulations, which was used to filter an in-house built virtual library of tetrapeptide ligands. The three top-scored compounds were synthesized and subjected to biological evaluation, revealing the identity of a hit compound (peptide 1) endowed with appreciable MOR inverse agonist effect and selectivity over δ-opioid receptors. These results confirmed the reliability of our computational approach and provided a promising starting point for the development of new potent MOR modulators. Full article
(This article belongs to the Special Issue Neuropeptides Involved in Pain Control)
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