Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin‑4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist

The melanocortin-4 receptor (MC4R) plays an important role in appetite. Agonist ligands that stimulate the MC4R decrease appetite, while antagonist compounds increase food consumption. Herein, a functional mixture-based positional scan identified novel MC4R antagonist sequences. Mixtures comprising...

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Veröffentlicht in:	Journal of medicinal chemistry 2021-10, Vol.64 (19), p.14860-14875
Hauptverfasser:	Ericson, Mark D, Doering, Skye R, Larson, Courtney M, Freeman, Katie T, LaVoi, Travis M, Donow, Haley M, Santos, Radleigh G, Cho, Rachel H, Koerperich, Zoe M, Giulianotti, Marc A, Pinilla, Clemencia, Houghten, Richard A, Haskell-Luevano, Carrie
Format:	Artikel
Sprache:	eng
Schlagworte:	Agouti-Related Protein - pharmacology Animals Complex Mixtures High-Throughput Screening Assays Humans Mice Oligopeptides - chemistry Oligopeptides - pharmacology Peptide Fragments - pharmacology Receptor, Melanocortin, Type 4 - drug effects Receptors, Melanocortin - drug effects Structure-Activity Relationship
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