Application of N-Dodecyl l-Peptide to Enhance Serum Stability while Maintaining Inhibitory Effects on Myometrial Contractions Ex Vivo

N-Alkylation and N-acylation of the prostaglandin-F(2α) allosteric modulator l-PDC31 were performed to install various alkyl, PEG and isoprenoid groups onto the l-enantiomer of the peptide. Among the different bio-conjugates studied, the N-dodecyl analog reduced prostaglandin-F(2α)-induced mouse myo...

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Detalles Bibliográficos
Autores principales: Poupart, Julien, Hou, Xin, Chemtob, Sylvain, Lubell, William D.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6891598/
https://www.ncbi.nlm.nih.gov/pubmed/31731725
http://dx.doi.org/10.3390/molecules24224141
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author Poupart, Julien
Hou, Xin
Chemtob, Sylvain
Lubell, William D.
author_facet Poupart, Julien
Hou, Xin
Chemtob, Sylvain
Lubell, William D.
author_sort Poupart, Julien
collection PubMed
description N-Alkylation and N-acylation of the prostaglandin-F(2α) allosteric modulator l-PDC31 were performed to install various alkyl, PEG and isoprenoid groups onto the l-enantiomer of the peptide. Among the different bio-conjugates studied, the N-dodecyl analog reduced prostaglandin-F(2α)-induced mouse myometrium contractions ex vivo. Furthermore, N-dodecyl-l-PDC31 exhibited improved stability in a mouse serum assay, likely due to protection from protease degradation by the lipid chain.
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spelling pubmed-68915982019-12-12 Application of N-Dodecyl l-Peptide to Enhance Serum Stability while Maintaining Inhibitory Effects on Myometrial Contractions Ex Vivo Poupart, Julien Hou, Xin Chemtob, Sylvain Lubell, William D. Molecules Article N-Alkylation and N-acylation of the prostaglandin-F(2α) allosteric modulator l-PDC31 were performed to install various alkyl, PEG and isoprenoid groups onto the l-enantiomer of the peptide. Among the different bio-conjugates studied, the N-dodecyl analog reduced prostaglandin-F(2α)-induced mouse myometrium contractions ex vivo. Furthermore, N-dodecyl-l-PDC31 exhibited improved stability in a mouse serum assay, likely due to protection from protease degradation by the lipid chain. MDPI 2019-11-15 /pmc/articles/PMC6891598/ /pubmed/31731725 http://dx.doi.org/10.3390/molecules24224141 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Poupart, Julien
Hou, Xin
Chemtob, Sylvain
Lubell, William D.
Application of N-Dodecyl l-Peptide to Enhance Serum Stability while Maintaining Inhibitory Effects on Myometrial Contractions Ex Vivo
title Application of N-Dodecyl l-Peptide to Enhance Serum Stability while Maintaining Inhibitory Effects on Myometrial Contractions Ex Vivo
title_full Application of N-Dodecyl l-Peptide to Enhance Serum Stability while Maintaining Inhibitory Effects on Myometrial Contractions Ex Vivo
title_fullStr Application of N-Dodecyl l-Peptide to Enhance Serum Stability while Maintaining Inhibitory Effects on Myometrial Contractions Ex Vivo
title_full_unstemmed Application of N-Dodecyl l-Peptide to Enhance Serum Stability while Maintaining Inhibitory Effects on Myometrial Contractions Ex Vivo
title_short Application of N-Dodecyl l-Peptide to Enhance Serum Stability while Maintaining Inhibitory Effects on Myometrial Contractions Ex Vivo
title_sort application of n-dodecyl l-peptide to enhance serum stability while maintaining inhibitory effects on myometrial contractions ex vivo
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6891598/
https://www.ncbi.nlm.nih.gov/pubmed/31731725
http://dx.doi.org/10.3390/molecules24224141
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