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Discovery Of Molecular Interactions Of The Human Melanocortin-4 Receptor (Hmc4r) Asp189 (D189) Amino Acid With The Endogenous G-Protein-Coupled Receptor (Gpcr) Antagonist Agouti-Related Protein (Agrp) Provides Insights To Agrp's Inverse Agonist Pharmacology At The Hmc4r, Mark D. Ericson, Erica M. Haslach, Sathya M. Schnell, Katie T. Freeman, Zhimin M. Xiang, Frederico P. Portillo, Robert Speth, Sally A. Litherland, Carrie Haskell-Luevano
Discovery Of Molecular Interactions Of The Human Melanocortin-4 Receptor (Hmc4r) Asp189 (D189) Amino Acid With The Endogenous G-Protein-Coupled Receptor (Gpcr) Antagonist Agouti-Related Protein (Agrp) Provides Insights To Agrp's Inverse Agonist Pharmacology At The Hmc4r, Mark D. Ericson, Erica M. Haslach, Sathya M. Schnell, Katie T. Freeman, Zhimin M. Xiang, Frederico P. Portillo, Robert Speth, Sally A. Litherland, Carrie Haskell-Luevano
HPD Articles
The melanocortin receptors (MCRs) are important for numerous biological pathways, including feeding behavior and energy homeostasis. In addition to endogenous peptide agonists, this receptor family has two naturally occurring endogenous antagonists, agouti and agouti-related protein (AGRP). At the melanocortin-4 receptor (MC4R), the AGRP ligand functions as an endogenous inverse agonist in the absence of agonist and as a competitive antagonist in the presence of agonist. At the melanocortin-3 receptor (MC3R), AGRP functions solely as a competitive antagonist in the presence of agonist. The molecular interactions that differentiate AGRP's inverse agonist activity at the MC4R have remained elusive until the findings …