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The melanocortin receptor subtypes in chicken have high preference to ACTH‐derived peptides
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Journal Article
The melanocortin receptor subtypes in chicken have high preference to ACTH‐derived peptides
2004
Overview
Melanocortin (MC) receptors are widely distributed throughout the body of chicken, like in mammals, and participate in a wide range of physiological functions. To clarify the pharmacological impact of ligands acting in the MC system, we expressed the chicken MC1, MC2, MC3, MC4 and MC5 (cMC1–5) receptors in eukaryotic cells and performed comprehensive pharmacological characterization of the potency of endogenous and synthetic melanocortin peptides. Remarkably, the cMC receptors displayed high affinity for ACTH‐derived peptides and in general low affinity for α‐MSH. It is evident that not only the cMC2 receptor but also the other cMC receptors interact with ACTH‐derived peptide through an epitope beyond the sequence of α‐MSH. The synthetic ligand MTII was found to be a potent agonist whereas HS024 was a potent antagonist at the cMC4 receptor, indicating that these ligands are suitable for physiological studies in chicken. We also show the presence of prohormone convertase 1 (PC1) and PC2 genes in chicken, and that these peptides are coexpressed with proopiomelanocortin (POMC) in various tissues. British Journal of Pharmacology (2004) 143, 626–637. doi:10.1038/sj.bjp.0705900
Publisher
Blackwell Publishing Ltd,Nature Publishing
Subject
/ Adrenocorticotropic Hormone - analogs & derivatives
/ Adrenocorticotropic Hormone - metabolism
/ Adrenocorticotropic Hormone - pharmacology
/ Animals
/ Binding, Competitive - drug effects
/ Biological and medical sciences
/ GPCR
/ Humans
/ Kinetics
/ MSH
/ Pharmacology. Drug treatments
/ Pro-Opiomelanocortin - metabolism
/ Proprotein Convertase 1 - genetics
/ Proprotein Convertase 1 - metabolism
/ Proprotein Convertase 2 - genetics
/ Proprotein Convertase 2 - metabolism
/ Receptors, Melanocortin - biosynthesis
/ Receptors, Melanocortin - drug effects
/ Receptors, Melanocortin - metabolism
