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Melanocortin activity

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https://www.readbyqxmd.com/read/28625749/preclinical-evaluation-of-melanocortin-1-receptor-mc1-r-specific-68-ga-and-44-sc-labeled-dota-napamide-in-melanoma-imaging
#1
Gábor Nagy, Noémi Dénes, Adrienn Kis, Judit P Szabó, Ervin Berényi, Ildikó Garai, Péter Bai, István Hajdu, Dezső Szikra, György Trencsényi
PURPOSE: Alpha melanocyte stimulating hormone (α-MSH) enhances melanogenesis in melanoma malignum by binding to melanocortin-1 receptors (MC1-R). Earlier studies demonstrated that alpha-MSH analog NAPamide molecule specifically binds to MC1-R receptor. Radiolabeled NAPamide is a promising radiotracer for the non-invasive detection of melanin producing melanoma tumors by Positron Emission Tomography (PET). In this present study the MC1-R selectivity of the newly developed Sc-44-labeled DOTA-NAPamide was investigated in vitro and in vivo using melanoma tumors...
June 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28614768/melanocortin-4-receptor-agonist-ro27-3225-ameliorates-soleus-but-not-gastrocnemius-atrophy-in-arthritic-rats
#2
A B Gomez-Sanmiguel, M P Nieto-Bona, C Fernandez-Galaz, T Priego, A I Martin, A Lopez-Calderon
Adjuvant-induced arthritis in rats decreases body weight and muscle mass. Melanocyte stimulating hormone administration to arthritic rats decreases inflammation and skeletal muscle wasting. In this study, we investigate whether activation of melanocortin-4 receptor by RO27-3225 administration is able to prevent the effect of arthritis on the expression of muscle-specific E3 ubiquitin ligases and MyoD in two different muscles, gastrocnemius (a mainly fast type muscle) and soleus (slow type). Arthritis was induced in male Wistar rats by intradermal injection of Freund's adjuvant...
April 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/28599948/fish-pigmentation-and-the-melanocortin-system
#3
REVIEW
Laura Cal, Paula Suarez-Bregua, José Miguel Cerdá-Reverter, Ingo Braasch, Josep Rotllant
The melanocortin system is a complex neuroendocrine signaling mechanism involved in numerous physiological processes in vertebrates, including pigmentation, steroidogenesis and metabolic control. This review focuses at one of its most fascinating function in fish, its regulatory role in the control of pigmentation, in which the melanocortin 1 receptor (Mc1r), its agonist α-melanocyte stimulating hormone (α-Msh), and the endogenous antagonist agouti signaling protein (Asip1) are the main players. Functional control of Mc1r, which is highly expressed in fish skin and whose activation stimulates melanin production and melanosome dispersion in fish melanophores, is considered a key mechanism for vertebrate pigment phenotypes...
June 7, 2017: Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology
https://www.readbyqxmd.com/read/28599303/oleoylethanolamide-inhibits-%C3%AE-melanocyte-stimulating-hormone-stimulated-melanogenesis-via-erk-akt-and-creb-signaling-pathways-in-b16-melanoma-cells
#4
Juan Zhou, Tong Ren, Ying Li, Anran Cheng, Wanyi Xie, Lanxi Xu, Lu Peng, Jinbin Lin, Lianxiang Lian, Yong Diao, Xin Jin, Lichao Yang
The present study aimed to examine the potential inhibitory activity of oleoylethanolamide (OEA) on α-melanocyte stimulating hormone (α-MSH)-stimulated melanogenesis and the molecular mechanism(s) involved in the process in B16 mouse melanoma cells. Our data demonstrated that OEA markedly inhibited melanin synthesis and tyrosinase activity in α-MSH-stimulated B16 cells. In addition, the expression of melanogenesis-related proteins, such as melanocortin-1 receptor (MC1R), microphthalmia-associated transcription factor (MITF), tyrosinase-related protein-1 (TRP-1) and tyrosinase, was suppressed in a concentration-dependent manner by OEA...
May 23, 2017: Oncotarget
https://www.readbyqxmd.com/read/28590933/the-caudal-pedunculopontine-tegmental-nucleus-may-be-involved-in-the-regulation-of-skeletal-muscle-activity-by-melanocortinsympathetic-pathway-a-virally-mediated-trans-synaptic-tracing-study-in-spinally-transected-transgenic-mice
#5
Zhi-Gang He, Bao-Wen Liu, Zhi-Xiao Li, Xue-Bi Tian, San-Guang Liu, Anne Manyande, Ding-Yu Zhang, Hong-Bing Xiang
Understanding neuroanatomical sympathetic circuitry and neuronal connections from the caudal pedunculopontine tegmental nucleus to skeletal muscle is important to the study of possible mechanisms of pedunculopontine tegmental nucleus (PPTg) and cuneiform nucleus (CnF) that are involved in the regulation of skeletal muscle activity of the sympathetic pathway. The aim of this study was to use virus PRV-614 to trace the melanocortin-sympathetic neural pathways from PPTg and CnF to a hindlimb muscle (gastrocnemius) in spinally transected MC4R-GFP transgenic mice...
May 18, 2017: Oncotarget
https://www.readbyqxmd.com/read/28579117/key-amino-acid-residue-in-melanocortin-1-receptor-melanocyte-%C3%AE-msh-receptor-for-ligand-selectivity
#6
Yingkui Yang, Min Chen, George Ventro, Carroll M Harmon
The melanocortin-1 receptor (MC1R) is a subtype of the melanocortin receptor family and NDP-α-MSH is a non-selective agonist for MC1R. The core sequence of NDP-α-MSH, His-Phe-Arg-Trp, is important for ligand binding and biological activities at the melanocortin receptor subtypes (MCRs). A recent study indicates that Trp(9) in NDP-α-MSH plays an important role in ligand selectivity. Deletion of Trp(9) in NDP-α-MSH (des-Trp(9)-NDP-α-MSH) resulted in loss of agonist activity at MC4R, although remains agonist activity at MC1R...
June 1, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28578648/synthetic-peptide-drugs-for-targeting-skin-cancer-malignant-melanoma-and-melanotic-lesions
#7
Alex Eberle, Bhimsen Rout, Mei Bigliardi Qi, Paul L Bigliardi
Peptides play decisive roles in the skin, ranging from host defense responses to various forms of neuroendocrine regulation of cell and organelle function. Synthetic peptides conjugated to radionuclides or photosensitizers may serve to identify and treat skin tumors and their metastatic forms in other organs of the body. In the introductory part of his review, the role and interplay of the different peptides in the skin is briefly summarized, including their potential application for the management of frequently occurring skin cancers...
June 4, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28575455/adolescent-alcohol-exposure-induced-changes-in-alpha-melanocyte-stimulating-hormone-and-neuropeptide-y-pathways-via-histone-acetylation-in-the-brain-during-adulthood
#8
Dadasaheb M Kokare, Evan J Kyzar, Huaibo Zhang, Amul J Sakharkar, Subhash C Pandey
Background: Adolescent intermittent ethanol (AIE) exposure causes long-lasting alterations in brain epigenetic mechanisms. Melanocortin and neuropeptide Y (NPY) signaling interact and are affected by ethanol exposure in the brain. Here, the persistent effects of AIE on alpha-melanocyte stimulating hormone (α-MSH), melanocortin 4 receptor (MC4R) and NPY expression and their regulation by histone acetylation mechanisms were investigated in adulthood. Methods: Male rats were exposed to AIE (2 g/kg, i...
May 31, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28551830/factors-responsible-for-obesity-related-hypertension
#9
REVIEW
Kyungjoon Lim, Kristy L Jackson, Yusuke Sata, Geoffrey A Head
PURPOSE OF REVIEW: The major health issue of being overweight or obese relates to the development of hypertension, insulin resistance and diabetic complications. One of the major underlying factors influencing the elevated blood pressure in obesity is increased activity of the sympathetic nerves to particular organs such as the kidney. RECENT FINDINGS: There is now convincing evidence from animal studies that major signals such as leptin and insulin have a sympathoexcitatory action in the hypothalamus to cause hypertension...
July 2017: Current Hypertension Reports
https://www.readbyqxmd.com/read/28551512/systemic-n-terminal-fragments-of-adrenocorticotropin-reduce-inflammation-and-stress-induced-anhedonia-in-rats
#10
Dmitrii D Markov, Ksenia A Yatsenko, Lyudmila S Inozemtseva, Igor A Grivennikov, Nikolai F Myasoedov, Oleg V Dolotov
Emerging evidence implicates impaired self-regulation of the hypothalamic-pituitary-adrenal (HPA) axis and inflammation as important and closely related components of the pathophysiology of major depression. Antidepressants show anti-inflammatory effects and are suggested to enhance glucocorticoid feedback inhibition of the HPA axis. HPA axis activity is also negatively self-regulated by the adrenocorticotropic hormone (ACTH), a potent anti-inflammatory peptide activating five subtypes of melanocortin receptors (MCRs)...
May 7, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28512117/the-interaction-of-mc3r-and-mc4r-with-mrap2-acth-%C3%AE-msh-and-agrp-in-chickens
#11
Jiannan Zhang, Xin Li, Yawei Zhou, Lin Cui, Jing Li, Chenlei Wu, Yiping Wan, Juan Li, Yajun Wang
The interaction of melanocortin-4 (MC4R) and melanocortin-3 (MC3R) receptors with proopiomelanocortin (POMC)-derived peptides (e.g. α-MSH), agouti-related protein (AgRP), and melanocortin-2 receptor accessory protein 2 (MRAP2) is suggested to play critical roles in energy balance of vertebrates. However, evidence on their interaction in birds remains scarce. Our study aims to reveal their interaction in chickens and the results showed that: 1) chicken (c-)MC3R and cMC4R expressed in CHO cells can be activated by α-MSH and ACTH1-39 equipotently, monitored by a pGL3-CRE-luciferase reporter system; 2) cMC3R and cMC4R, when co-expressed with cMRAP2 (or cMRAP, a cMRAP2 homolog), show increased sensitivity to ACTH treatment and thus likely act as ACTH-preferring receptors, and the interaction between cMC3R/cMC4R and cMRAP2 was demonstrated by co-immunoprecipitation assay; 3) both cMC3R and cMC4R display constitutive activity when expressed in CHO cells, as monitored by Dual-luciferase reporter assay, and cMRAP2 (and cMRAP) can modulate their constitutive activity; 4) AgRP inhibits the constitutive activity of cMC3R/cMC4R, and it also antagonizes ACTH/α-MSH action on cMC4R/cMC3R, indicating that AgRP functions as the inverse agonist and antagonist for both receptors...
May 16, 2017: Journal of Endocrinology
https://www.readbyqxmd.com/read/28507313/chronic-intrahypothalamic-rather-than-subcutaneous-liraglutide-treatment-reduces-body-weight-gain-and-stimulates-the-melanocortin-receptor-system
#12
K Kaineder, T Birngruber, G Rauter, B Obermüller, J Eichler, J Münzker, W Al-Zoughbi, S I Mautner, S S Torekov, B Hartmann, P Kotzbeck, T R Pieber
BACKGROUND: The GLP-1 receptor agonist liraglutide is marketed for obesity treatment where it induces body weight reduction possibly via the hypothalamus, which regulates energy homeostasis. In animal studies, acute liraglutide treatment triggers satiety, weight loss and activates thermogenesis in adipose tissue. However, the precise mechanisms how liraglutide affects in particular chronic weight loss are still under investigation. OBJECTIVES: We aimed to evaluate whether chronic hypothalamic or chronic subcutaneous administration of liraglutide induces sustained weight loss through altered adipose tissue function and to what extent hypothalamic neuronal appetite regulators are involved in the liraglutide-induced weight loss in healthy lean rats on a normal diet...
April 25, 2017: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/28500249/maternal-high-fat-diet-induces-metabolic-stress-response-disorders-in-offspring-hypothalamus
#13
Long The Nguyen, Sonia Saad, Yi Tan, Carol Pollock, Hui Chen
Maternal obesity has been shown to increase the risk of obesity and related disorders in the offspring, which has been partially attributed to changes of appetite regulators in the offspring hypothalamus. On the other hand, endoplasmic reticulum (ER) stress and autophagy have been implicated in hypothalamic neuropeptide dysregulation, thus may also play important roles in such transgenerational effect.  In this study, we show that offspring born to HFD-fed dams showed significantly increased body weight and glucose intolerance, adiposity and plasma triglyceride level at weaning...
May 12, 2017: Journal of Molecular Endocrinology
https://www.readbyqxmd.com/read/28499989/melanocortin-receptor-accessory-proteins-mraps-functions-in-the-melanocortin-system-and-beyond
#14
REVIEW
Alix A J Rouault, Dinesh K Srinivasan, Terry C Yin, Abigail A Lee, Julien A Sebag
G-protein coupled receptors (GPCRs) are regulated by numerous proteins including kinases, G-proteins, β-arrestins and accessory proteins. Several families of GPCR accessory proteins like Receptor Activity Modifying Proteins, Receptor Transporting Proteins and Melanocortin Receptor Accessory Proteins (MRAPs) have been identified as regulator of receptor trafficking, signaling and ligand specificity. The MRAP family contains two members, MRAP1 and MRAP2, responsible for the formation of a functional ACTH receptor and for the regulation of energy homeostasis respectively...
May 9, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28495271/the-melanocortin-2-receptor-of-the-rainbow-trout-identifying-a-role-for-critical-positions-in-transmembrane-domain-4-extracellular-loop-2-and-transmembrane-domain-5-in-the-activation-of-rainbow-trout-mc2r
#15
Liang Liang, Perry V Davis, Michael R Dores, Robert M Dores
The activation of either teleost or tetrapod melanocortin-2 receptor (MC2R) orthologs requires interaction between the HFRW motif and R/KKRRP motif in the primary sequence of ACTH, and two corresponding sites on the melanocortin 2 receptor. While the HFRW contact site on MC2R appears to involve residues in TM2, TM3, and TM6, several studies on human MC2R point to the EC2/TM5 region of MC2R as a possible location for the R/KKRRP contact site. In this study nineteen single-alanine mutants of rainbow trout (rt) MC2R were made beginning at V(153) in TM4, at all positions in EC2 (extracellular loop 2), to F(175) in TM5...
May 8, 2017: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28491052/receptor-mediated-melanoma-targeting-with-radiolabeled-%C3%AE-melanocyte-stimulating-hormone-relevance-of-the-net-charge-of-the-ligand
#16
Jean-Philippe Bapst, Alex N Eberle
A majority of melanotic and amelanotic melanomas overexpress melanocortin type 1 receptors (MC1Rs) for α-melanocyte-stimulating hormone. Radiolabeled linear or cyclic analogs of α-MSH have a great potential as diagnostic or therapeutic tools for the management of malignant melanoma. Compounds such as [(111)In]DOTA-NAP-amide exhibit high affinity for the MC1R in vitro, good tumor uptake in vivo, but they may suffer from relatively high kidney uptake and retention in vivo. We have shown previously that the introduction of negative charges into radiolabeled DOTA-NAP-amide peptide analogs may enhance their excretion and reduce kidney retention...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28452072/pgc-1%C3%AE-in-melanoma-a-key-factor-for-antioxidant-response-and-mitochondrial-function
#17
Margalida Torrens-Mas, Daniel González-Hedström, Marta Abrisqueta, Pilar Roca, Jordi Oliver, Jorge Sastre-Serra
Melanocortin 1 receptor (MC1R) and BRAF are common mutations in melanoma. Through different pathways, they each regulate the expression of PGC-1α, which is a key factor in the regulation of mitochondrial biogenesis and the antioxidant response. Our aim was to study the importance of the different regulatory characteristics of MC1R and BRAF on the pathways they regulate in melanoma. For this purpose, ROS production, levels of gene expression and enzymatic activities were analyzed in HBL and MeWo, with wild-type MC1R and BRAF, and A375 cells with mutant MC1R and BRAF...
April 27, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28450851/regulation-of-agouti-related-protein-and-pro-opiomelanocortin-gene-expression-in-the-avian-arcuate-nucleus
#18
REVIEW
Timothy Boswell, Ian C Dunn
The arcuate nucleus is generally conserved across vertebrate taxa in its neuroanatomy and neuropeptide expression. Gene expression of agouti-related protein (AGRP), neuropeptide Y (NPY), pro-opiomelanocortin (POMC), and cocaine- and amphetamine-regulated transcript (CART) has been established in the arcuate nucleus of several bird species and co-localization demonstrated for AGRP and NPY. The proteins encoded by these genes exert comparable effects on food intake in birds after central administration to those seen in other vertebrates, with AGRP and NPY being orexigenic and CART and α-melanocyte-stimulating hormone anorexigenic...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28450348/melanocortin-1-receptor-signaling-regulates-cholesterol-transport-in-macrophages
#19
Petteri Rinne, Martina Rami, Salla L Nuutinen, Donato Santovito, Emiel P C van der Vorst, Raquel Guillamat-Prats, Leo-Pekka Lyytikäinen, Emma Raitoharju, Niku Oksala, Larisa Ring, Minying Cai, Victor J Hruby, Terho J Lehtimäki, Christian Weber, Sabine Steffens
Background -The melanocortin 1 receptor (MC1-R) is expressed by monocytes and macrophages, where it exerts anti-inflammatory actions upon stimulation with its natural ligand α-melanocyte-stimulating hormone (α-MSH). The present study was designed to investigate the specific role of MC1-R in the context of atherosclerosis and possible regulatory pathways of MC1-R beyond anti-inflammation. Methods -Human and mouse atherosclerotic samples and primary mouse macrophages were used to study the regulatory functions of MC1-R...
April 27, 2017: Circulation
https://www.readbyqxmd.com/read/28438719/chick-subcutaneous-and-abdominal-adipose-tissue-depots-respond-differently-in-lipolytic-and-adipogenic-activity-to-%C3%AE-melanocyte-stimulating-hormone-%C3%AE-msh
#20
Steven L Shipp, Guoqing Wang, Mark A Cline, Elizabeth R Gilbert
In birds, α-MSH is anorexigenic, but effects on adipose tissue are unknown. Four day-old chicks were intraperitoneally injected with 0 (vehicle), 5, 10, or 50μg of α-MSH and subcutaneous and abdominal adipose tissue collected at 60min for RNA isolation (n=10). Plasma was collected post-euthanasia at 60 and 180min for measuring non-esterified fatty acids (NEFA) and α-MSH (n=10). Relative to the vehicle, food intake was reduced in the 50μg-treated group. Plasma NEFAs were greater in 10μg than vehicle-treated chicks at 3h...
July 2017: Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology
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