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Synergistic Multi-Residue Substitutions of a Macrocyclic c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro] Agouti-Related Protein (AGRP) Scaffold Yield Potent and >600-Fold MC4R versus MC3R Selective Melanocortin Receptor Antagonists
Antagonist ligands of the melanocortin-3 and −4 receptors (MC3R, MC4R), including agouti-related protein (AGRP), are postulated to be targets for the treatment of diseases of negative energy balance. Previous studies reported the macrocyclic MC3R/MC4R antagonist c[Pro(1)−Arg(2)−Phe(3)−Phe(4)−Asn(5)−...
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| Publicado no: | J Med Chem |
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| Main Authors: | , , , |
| Formato: | Artigo |
| Idioma: | Inglês |
| Publicado em: |
2018
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| Assuntos: | |
| Acesso em linha: | https://ncbi.nlm.nih.gov/pmc/articles/PMC6174881/ https://ncbi.nlm.nih.gov/pubmed/30035543 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b00684 |
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