Abstract
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.
| Original language | English |
|---|---|
| Pages (from-to) | 626-637 |
| Number of pages | 12 |
| Journal | British Journal of Pharmacology |
| Volume | 143 |
| Issue number | 5 |
| DOIs | |
| Publication status | Published - Nov 2004 |
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Keywords
- ACTH
- GPCR
- MC receptor subtypes
- MSH
ASJC Scopus subject areas
- Pharmacology
Cite this
The melanocortin receptor subtypes in chicken have high preference to ACTH-derived peptides. / Ling, Maria K.; Hotta, Eri; Kilianova, Zuzana; Haitina, Tatjana; Ringholm, Aneta; Johansson, Lisa; Gallo-Payet, Nicole; Takeuchi, Sakae; Schiöth, Helgi B.
In: British Journal of Pharmacology, Vol. 143, No. 5, 11.2004, p. 626-637.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - The melanocortin receptor subtypes in chicken have high preference to ACTH-derived peptides
AU - Ling, Maria K.
AU - Hotta, Eri
AU - Kilianova, Zuzana
AU - Haitina, Tatjana
AU - Ringholm, Aneta
AU - Johansson, Lisa
AU - Gallo-Payet, Nicole
AU - Takeuchi, Sakae
AU - Schiöth, Helgi B.
PY - 2004/11
Y1 - 2004/11
N2 - 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.
AB - 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.
KW - ACTH
KW - GPCR
KW - MC receptor subtypes
KW - MSH
UR - http://www.scopus.com/inward/record.url?scp=8744273696&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=8744273696&partnerID=8YFLogxK
U2 - 10.1038/sj.bjp.0705900
DO - 10.1038/sj.bjp.0705900
M3 - Article
VL - 143
SP - 626
EP - 637
JO - British Journal of Pharmacology
JF - British Journal of Pharmacology
SN - 0007-1188
IS - 5
ER -