Application of <i>N</i>-Dodecyl <span style="font-variant: small-caps">l</span>-Peptide to Enhance Serum Stability while Maintaining Inhibitory Effects on Myometrial Contractions Ex Vivo
oleh: Julien Poupart, Xin Hou, Sylvain Chemtob, William D. Lubell
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2019-11-01 |
Deskripsi
<i>N</i>-Alkylation and <i>N</i>-acylation of the prostaglandin-F<sub>2α</sub> allosteric modulator <span style="font-variant: small-caps;">l</span>-PDC31 were performed to install various alkyl, PEG and isoprenoid groups onto the <span style="font-variant: small-caps;">l</span>-enantiomer of the peptide. Among the different bio-conjugates studied, the <i>N</i>-dodecyl analog reduced prostaglandin-F<sub>2α</sub>-induced mouse myometrium contractions ex vivo. Furthermore, <i>N</i>-dodecyl-<span style="font-variant: small-caps;">l</span>-PDC31 exhibited improved stability in a mouse serum assay, likely due to protection from protease degradation by the lipid chain.