Related Experiment Video
Updated: Jul 3, 2025

Development of Recombinant Proteins to Treat Chronic Pain
Published on: April 11, 2018
Stapling of leu-enkephalin analogs with bifunctional reagents for prolonged analgesic activity
Monika Kijewska1, Grzegorz Wołczański1, Piotr Kosson2
1Faculty of Chemistry, University of Wrocław, Joliot-Curie 14, 50-383 Wrocław, Poland. monika.kijewska@uwr.edu.pl.
Abstract:
The design and synthesis of leu-enkephalin analogs by replacing the glycine residues with N-(2-thioethyl)glycines and opening the cyclisation potential is presented. The cyclization (stapling) was achieved using bifunctional reagents (hexafluorobenzene and trithiocyanuric acid derivatives). The CD conformational studies of the stapled analogs suggest that the peptides adopt the type I β-turn conformation, which is in agreement with the theoretical analysis. The analog containing a trithiocyanuric acid derivative with a benzyl substituent shows potent analgesic activity.
Related Concept Videos
Opioid Analgesics: Synthetic and Semisynthetic Opioids
Analgesia and Pain Management
Local Anesthetics: Chemistry and Structure-Activity Relationship
Local Anesthetics: Clinical Application as Epidural Anesthesia
Since epidural anesthetics can be infused through an epidural catheter, all types of drugs, including short-acting ones, can be administered. Chloroprocaine and lidocaine are examples of short and long-duration anesthetics, respectively. Bupivacaine...
Local Anesthetics: Mechanism of Action
Local anesthetics are amphiphilic molecules consisting of a hydrophobic aromatic part linked to a hydrophilic group by an ester or amide linkage. They are weak bases and are usually available as salts, which increases their solubility and stability. Once administered, LAs exist in the body either...
Local Anesthetics: Pharmacokinetics

