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Application Of N-Dodecyl L-Peptide To Enhance Serum Stability While Maintaining Inhibitory Effects On Myometrial Contractions Ex Vivo

Julien Poupart, Xin Hou, Sylvain Chemtob, William D. Lubell

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N-Alkylation and N-acylation of the prostaglandin-F2α 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-F2α-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.