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Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AGRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin-5 Receptor Antagonists

While the melanocortin receptors (MCRs) are known to be involved in numerous biological pathways, the potential roles of the MC5R have not been clearly elucidated in humans. AgRP, an MC3R/MC4R antagonist and MC4R inverse agonist, contains an exposed ß-hairpin loop composed of six residues (Arg-Phe-P...

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Dades bibliogràfiques
Publicat a:J Med Chem
Autors principals: Koerperich, Zoe M., Ericson, Mark D., Freeman, Katie T., Speth, Robert C., Pogozheva, Irina D., Mosberg, Henry I., Haskell-Luevano, Carrie
Format: Artigo
Idioma:Inglês
Publicat: 2020
Matèries:
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC7250496/
https://ncbi.nlm.nih.gov/pubmed/31845801
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b00860
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