Structure, function and regulation of the melanocortin receptors [PDF]
Melanocortin receptors belong to the seven-transmembrane (TM) domain proteins that are coupled to G-proteins and signaled through intracellular cyclic adenosine monophosphate. Many structural features conserved in other G-protein coupled receptors (GPCRs) are found in the melanocortin receptors. There are five melanocortin receptor subtypes and each of
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Loss-of-function mutations in the melanocortin-2-receptor (mc2r) lead to skin hyperpigmentation in teleost fish [PDF]
Melanocortins regulate pigmentation via melanocortin receptors (MCRs), which are highly conserved across vertebrates. Unlike other MCRs, the melanocortin 2 receptor (MC2R) is exclusively activated by ACTH; however, its role in pigmentation remains ...
Elisa Barreiro-Docío +9 more
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“Are melanocortin receptors constitutively active in vivo?” [PDF]
Constitutive activity is defined as ligand-independent activity, resulting in the production of a second messenger, even in the absence of an agonist. There has been widespread acceptance of the concept of G-protein-coupled receptor constitutive activity, with this activity specifically blocked by inverse agonists, a particular class of ligands often ...
Coll, Anthony P.
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Melanocortin System in Kidney Homeostasis and Disease: Novel Therapeutic Opportunities
Melanocortin peptides, melanocortin receptors, melanocortin receptor accessory proteins, and endogenous antagonists of melanocortin receptors are the key components constituting the melanocortin hormone system, one of the most complex and important ...
Mingyang Chang +4 more
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Melanocortin receptor 3 and 4 mRNA expression in the adult female Syrian hamster brain
Melanocortin 3 receptors (MC3R) and melanocortin 4 receptors (MC4R) are vital in regulating a variety of functions across many species. For example, the dysregulation of these receptors results in obesity and dysfunction in sexual behaviors.
Megan A. L. Hall +6 more
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Identification of novel GPCR partners of the central melanocortin signaling
Objective: Homo- or heterodimerization of G protein–coupled receptors (GPCRs) generally alters the normal functioning of these receptors and mediates their responses to a variety of physiological stimuli in vivo.
Yunpeng Li +13 more
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Melanocortin receptors in GtoPdb v.2021.3 [PDF]
Melanocortin receptors (provisional nomenclature as recommended by NC-IUPHAR [41]) are activated by members of the melanocortin family (α-MSH, β-MSH and γ-MSH forms; δ form is not found in mammals) and adrenocorticotrophin (ACTH ...
Gantz, Ira +14 more
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Evolutionary aspects in evaluating mutations in the melanocortin 4 receptor [PDF]
More than 70 missense mutations have been identified in the human melanocortin 4 receptor (MC4R), and many of them have been associated with obesity. In a number of cases, the causal link between mutations in MC4R and obesity is controversially discussed.
Stäubert, Claudia +17 more
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Novel anti-inflammatory and chondroprotective effects of the human melanocortin MC1 receptor agonist BMS-470539 dihydrochloride and human melanocortin MC3 receptor agonist PG-990 on lipopolysaccharide activated chondrocytes [PDF]
Human melanocortin MC1 and MC3 receptors expressed on C-20/A4 chondrocytes exhibit chondroprotective and anti-inflammatory effects when activated by melanocortin peptides.
De Pascale, C. +15 more
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Melanocortins and agouti-related protein modulate the excitability of two arcuate nucleus neuron populations by alteration of resting potassium conductances [PDF]
The hypothalamic melanocortin system is crucial for the control of appetite and body weight. Two of the five melanocortin receptors, MC3R and MC4R are involved in hypothalamic control of energy homeostasis, with the MC4R having the major influence. It is
Hisadome, Kazunari +11 more
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