Constitutive receptor activity series: endogenous inverse agonists and constitutive receptor activity in the melanocortin system.

Abstract

The recent discovery of melanocortin receptor mutations that selectively decrease constitutive receptor activity in obese individuals supports the physiological relevance of constitutive melanocortin receptor activity and its control by an endogenous inverse agonist. Furthermore, studies using mice that lack endogenous melanocortin receptor agonists show that differences in coat color are caused by different degrees of constitutive melanocortin receptor signaling regulated by an endogenous inverse agonist. Thus, the regulation of constitutive activity of melanocortin receptors is important for the normal control of pigmentation and body-weight homeostasis.

• Authors: Roger A H Adan
• Journal: Trends in pharmacological sciences (Trends Pharmacol Sci) Vol. 27 Issue 4 Pg. 183-6 (Apr 2006) ISSN: 0165-6147 [Print] England
• PMID: 16500715 (Publication Type: Journal Article)

Chemical References

• Agouti Signaling Protein
• Agouti-Related Protein
• Intercellular Signaling Peptides and Proteins
• Ligands
• Proteins
• Receptor, Melanocortin, Type 4
• Receptors, Melanocortin
• Melanocyte-Stimulating Hormones

Topics

• Agouti Signaling Protein
• Agouti-Related Protein
• Amino Acid Sequence
• Animals
• Humans
• Intercellular Signaling Peptides and Proteins (biosynthesis, physiology)
• Ligands
• Melanocyte-Stimulating Hormones (agonists, antagonists & inhibitors)
• Melanocytes (metabolism)
• Molecular Sequence Data
• Mutation
• Neurons (metabolism)
• Obesity (genetics, metabolism)
• Pigmentation (genetics)
• Proteins (physiology)
• Receptor, Melanocortin, Type 4 (agonists, genetics, metabolism)
• Receptors, Melanocortin (genetics, metabolism)