Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at the Melanocortin-5 Receptor

The melanocortin system consists of five reported receptors, agonists from the proopiomelanocortin gene transcript, and two antagonists, agouti-signaling protein (ASP) and agouti-related protein (AGRP). For both ASP and AGRP, the hypothesized Arg-Phe-Phe pharmacophores are on exposed β-hairpin loops...

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Veröffentlicht in:J Med Chem
Hauptverfasser: Ericson, Mark D., Freeman, Katie T., Schnell, Sathya M., Fleming, Katlyn A., Haskell-Luevano, Carrie
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2017
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5645029/
https://ncbi.nlm.nih.gov/pubmed/28813605
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.7b00856
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