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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...
Αποθηκεύτηκε σε:
| Τόπος έκδοσης: | J Med Chem |
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| Κύριοι συγγραφείς: | , , , , , , , , , , |
| Μορφή: | Artigo |
| Γλώσσα: | Inglês |
| Έκδοση: |
2016
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| Θέματα: | |
| Διαθέσιμο Online: | 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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