Side chain cyclized aromatic amino acids: great tools as local constraints in peptide and peptidomimetic design
O Van der Poorten, A Knuhtsen… - Journal of Medicinal …, 2016 - ACS Publications
Constraining the conformation of flexible peptides is a proven strategy to increase potency,
selectivity, and metabolic stability. The focus has mostly been on constraining the backbone …
selectivity, and metabolic stability. The focus has mostly been on constraining the backbone …
Biological evaluation and molecular docking studies of AA3052, a compound containing a μ-selective opioid peptide agonist DALDA and d-Phe-Phe-d-Phe-Leu-Leu …
A Kowalczyk, P Kleczkowska, M Rękawek… - European Journal of …, 2016 - Elsevier
The design of novel drugs for pain relief with improved analgesic properties and diminished
side effect induction profile still remains a challenging pursuit. Tolerance is one of the most …
side effect induction profile still remains a challenging pursuit. Tolerance is one of the most …
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs
A Adamska, A Kluczyk, MC Cerlesi, G Calo… - Bioorganic & Medicinal …, 2016 - Elsevier
Abstract Morphiceptin (Tyr-Pro-Phe-Pro-NH 2), a tetrapeptide amide, is a selective ligand of
the μ-opioid receptor (MOR). This study reports the synthesis and biological evaluation of a …
the μ-opioid receptor (MOR). This study reports the synthesis and biological evaluation of a …
Conformationally constrained peptidomimetics as inhibitors of the protein arginine methyl transferases
A Knuhtsen, B Legrand… - … A European Journal, 2016 - Wiley Online Library
Protein arginine N‐methyl transferases (PRMTs) belong to a family of enzymes that
modulate the epigenetic code through modifications of histones. In the present study …
modulate the epigenetic code through modifications of histones. In the present study …