Discovery of Kynurenines Containing Oligopeptides as Potent Opioid Receptor Agonists.

Clicks: 372
ID: 96067
2020
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Abstract
Kynurenine (kyn) and kynurenic acid (kyna) are well-defined metabolites of tryptophan catabolism collectively known as "kynurenines", which exert regulatory functions in host-microbiome signaling, immune cell response, and neuronal excitability. Kynurenine containing peptides endowed with opioid receptor activity have been isolated from natural organisms; thus, in this work, novel opioid peptide analogs incorporating L-kynurenine (L-kyn) and kynurenic acid (kyna) in place of native amino acids have been designed and synthesized with the aim to investigate the biological effect of these modifications. The kyna-containing peptide () binds selectively the m-opioid receptor with a Ki = 1.08 ± 0.26 (selectivity ratio m/d/k = 1:514:10000), while the L-kyn-containing peptide () shows a mixed binding affinity for m, d, and k-opioid receptors, with efficacy and potency (E = 209.7 + 3.4%; LogEC = -5.984 + 0.054) higher than those of the reference compound DAMGO. This novel oligopeptide exhibits a strong antinociceptive effect after i.c.v. and s.c. administrations in in vivo tests, according to good stability in human plasma (t = 47 min).
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szcs2020discoverybiomolecules Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Edina Szűcs, Azzurra Stefanucci, Marilisa Pia Dimmito, Ferenc Zádor, Stefano Pieretti, Gokhan Zengin, László Vécsei, Sándor Benyhe, Marianna Nalli, Adriano Mollica
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Journal Biomolecules
Year 2020
DOI
E284
URL
Keywords
peptides pharmacophore binding affinity g-protein activation kynurenines μ-opioid receptor

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