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
Descripción
Sumario: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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