Constitutive receptor activity series: endogenous inverse agonists and constitutive receptor activity in the melanocortin system.
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.
Adan
Roger A H
RA
Rudolf Magnus Institute of Neuroscience, Department of Pharmacology and Anatomy, University Medical Center Utrecht, PO Box 85060, 3508 AB, Utrecht, The Netherlands. r.a.h.adan@med.uu.nl
D054366:Agouti Signaling Protein; D054369:Agouti-Related Protein; D000595:Amino Acid Sequence; D000818:Animals; D006801:Humans; D036341:Intercellular Signaling Peptides and Proteins / Q000096:biosynthesis / Q000502:physiology*; D008024:Ligands; D009074:Melanocyte-Stimulating Hormones / Q000819:agonists / Q000037:antagonists & inhibitors*; D008544:Melanocytes / Q000378:metabolism; D008969:Molecular Sequence Data; D009154:Mutation; D009474:Neurons / Q000378:metabolism; D009765:Obesity / Q000235:genetics / Q000378:metabolism; D010858:Pigmentation / Q000235:genetics; D011506:Proteins / Q000502:physiology; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists / Q000235:genetics / Q000378:metabolism*; D044101:Receptors, Melanocortin / Q000235:genetics / Q000378:metabolism*
D054366:Agouti Signaling Protein; D054369:Agouti-Related Protein; D036341:Intercellular Signaling Peptides and Proteins; D008024:Ligands; D011506:Proteins; D044105:Receptor, Melanocortin, Type 4; D044101:Receptors, Melanocortin; D009074:Melanocyte-Stimulating Hormones