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Trifluoromethylthio and trifluoromethyl functionalization of endomorphin-1 enhances its hydrophobicity and plasma stability while preserving its affinity for the [mu]-opioid receptor
Jure Gregorc, Jolien De Neve, Karine Guitot, Brian J. Holleran, Nathalie Lensen, Louis Gendron, Thierry Brigaud, Jernej Iskra, Steven Ballet, Grégory Chaume
Izvirni znanstveni članek
Oznake: ligandi;peptidi;opioidni receptorji;fluor;metabolna stabilnost;ligands;peptides;opioid receptors;fluorine;metabolic stability;
The incorporation of fluorinated amino acid residues into peptides represents a promising strategy for improving the pharmacokinetic properties of bioactive peptides. Herein, we report the solid-phase synthesis (SPPS) of a set of ten SCF$_{3^-}$ or CF$_{3^-}$ modified neuropeptide analogs based on e ...
Leto: 2026 Vir: Fakulteta za kemijo in kemijsko tehnologijo (UL FKKT)
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