Peptides 101 (2018) 227–233 Contents lists available at ScienceDirect Peptides journal homepage: www.elsevier.com/locate/peptides Cyclopeptide Dmt-[D-Lys-p-CF -Phe-Phe-Asp]NH , a novel G protein-biased 3 2 agonist of the mu opioid receptor a b b a, Justyna Piekielna-Ciesielska , Federica Ferrari , Girolamo Calo’ , Anna Janecka Department of Biomolecular Chemistry, Faculty of Medicine, Medical University of Lodz, Lodz, Poland Department of Medical Sciences, Section of Pharmacology and Italian Institute of Neuroscience, University of Ferrara, 44121 Ferrara, Italy ARTICLE I NFO ABSTRACT Keywords: Opioid peptides and alkaloid drugs such as morphine, mediate their analgesic eﬀects, but also undesired side Opioid receptors eﬀects, mostly through activation of the mu opioid receptor which belongs to the G protein-coupled receptor Opioid peptides (GPCR) family. A new important pharmacological concept in the ﬁeld of GPCRs is biased agonism. Two mu Biased analogs receptor ligands, Dmt-c[D-Lys-Phe-Phe-Asp]NH (C-36) and Dmt-c[D-Lys-Phe-p-CF -Phe-Asp]NH (F-81), were 2 3 2 G protein-coupled receptors evaluated in terms of their ability to promote or block mu receptor/G protein and mu receptor/β-arrestin in- β-Arrestins teractions. Using the bioluminescence resonance energy transfer (BRET) assay it was shown that C-36 activated Bioluminescence resonance energy transfer both, G protein and β-arrestin pathways. Incorporation of triﬂuoromethyl group into the
Peptides – Elsevier
Published: Mar 1, 2018
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