A Cyclic Tetrapeptide (“Cyclodal”) and Its Mirror-Image Isomer Are Both High-Affinity μ Opioid Receptor Antagonists

[Image: see text] Head-to-tail cyclization of the μ opioid receptor (MOR) agonist [Dmt(1)]DALDA (H-Dmt-d-Arg-Phe-Lys-NH(2) (9; Dmt = 2′,6′-dimethyltyrosine) resulted in a highly active, selective MOR antagonist, c[-d-Arg-Phe-Lys-Dmt-] (1) (“cyclodal”), with subnanomolar binding affinity. A docking s...

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Publicat a:J Med Chem
Autors principals: Weltrowska, Grazyna, Nguyen, Thi M.-D., Chung, Nga N., Wood, JodiAnne, Ma, Xiaoyu, Guo, Jason, Wilkes, Brian C., Ge, Yang, Laferrière, André, Coderre, Terence J., Schiller, Peter W.
Format: Artigo
Idioma:Inglês
Publicat: 2016
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Article
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC5222732/
https://ncbi.nlm.nih.gov/pubmed/27676089
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01200
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