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melanocortin receptor

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https://www.readbyqxmd.com/read/28727208/differential-expression-of-appetite-regulating-genes-in-avian-models-of-anorexia-and-obesity
#1
Jiaqing Yi, Jingwei Yuan, Elizabeth R Gilbert, Paul B Siegel, Mark A Cline
Chickens from lines that have been selected for low (LWS) or high (HWS) juvenile body weight for more than 57 generations provide a unique model to research appetite regulation. The LWS display different severities of anorexia while all HWS become obese. Herein we measured mRNA abundance of various factors in appetite-associated nuclei in the hypothalamus. The lateral hypothalamus (LHA), paraventricular nucleus (PVN), ventromedial hypothalamus (VMH), dorsomedial nucleus (DMN), and arcuate nucleus (ARC) were collected from 5 day-old chicks that were fasted for 180 minutes or provided continuous access to food...
July 20, 2017: Journal of Neuroendocrinology
https://www.readbyqxmd.com/read/28720755/functional-variants-of-the-melanocortin-4-receptor-associated-with-the-odontoceti-and-mysticeti-suborders-of-cetaceans
#2
Liyuan Zhao, Xiaofan Zhou, Antonis Rokas, Roger D Cone
Cetaceans, a group of mammals adapted to the aquatic environment that descended from terrestrial artiodactyls, exhibit tremendous interspecific differences in a number of phenotypes, including feeding behavior, such as filter feeding in the Mysticeti vs prey-hunting Odontoceti, and size, with the smallest cetacean, the vaquita, at 1.4 meters and the largest, the blue whale, reaching 33 meters. The Melanocortin-4 receptor (MC4R) regulates food intake, energy balance, and somatic growth in both mammals and teleosts...
July 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28715181/structural-insights-into-selective-ligand-receptor-interactions-leading-to-receptor-inactivation-utilizing-selective-melanocortin-3-receptor-antagonists
#3
Minying Cai, Udaya Kiran Marelli, Blake Mertz, Johannes G Beck, Florian Opperer, Florian Rechenmacher, Horst Kessler, Victor J Hruby
Systematic N-methylated derivatives of the melanocortin receptor ligand, SHU9119, lead to mul-tiple binding and functional selectivity towards melanocortin receptors. However, the relationship between N-methylation-induced conformational changes in the peptide backbone and side chains and melanocortin receptor selectivity is still unknown. We conducted comprehensive conforma-tional studies in solution of two selective antagonists of the third isoform of the melanocortin re-ceptor (hMC3R), namely, Ac-Nle-c[Asp-NMe-His6-D-Nal(2')7-NMe-Arg8-Trp9-Lys]-NH2 (15) and Ac-Nle-c[Asp-His6-D-Nal(2')7-NMe-Arg8-NMe-Trp9-NMe-Lys]-NH2 (17)...
July 17, 2017: Biochemistry
https://www.readbyqxmd.com/read/28714883/nmr-insights-into-the-structure-function-relationships-in-the-binding-of-melanocortin-analogues-to-the-mc1r-receptor
#4
Maurício Morais, Héctor Zamora-Carreras, Paula D Raposinho, Maria Cristina Oliveira, David Pantoja-Uceda, João D G Correia, M Angeles Jiménez
Linear and cyclic analogues of the α-melanocyte stimulating hormone (α-MSH) targeting the human melanocortin receptor 1 (MC1R) are of pharmacological interest for detecting and treating melanoma. The central sequence of α-MSH (His-Phe-Arg-Trp) has been identified as being essential for receptor binding. To deepen current knowledge on the molecular basis for α-MSH bioactivity, we aimed to understand the effect of cycle size on receptor binding. To that end, we synthesised two macrocyclic isomeric α-MSH analogues, c[NH-NO₂-C₆H₃-CO-His-DPhe-Arg-Trp-Lys]-Lys-NH₂ (CycN-K6) and c[NH-NO₂-C₆H₃-CO-His-DPhe-Arg-Trp-Lys-Lys]-NH₂ (CycN-K7)...
July 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28699792/novel-approaches-to-the-design-of-bioavailable-melanotropins
#5
Yang Zhou, Minying Cai
The melanocortin system is a primordial and critical system for survival, involved in a wide variety of physiological functions. It includes melanocortin receptors (MCRs) and melanotropin ligands (MCLs). MCRs are important drug targets that can regulate several key physiological processes. Extensive efforts have been made to develop peptide and peptidomimetics targeting melanocortin receptors including MC1R, MC3R, MC4R and MC5R. Most research is focused on developing potent and selective melanotropins. However, developing bioavailable melanotropins remains challenging...
July 12, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28677151/getting-a-tan-without-getting-sik
#6
John D'Orazio
It has been more than a decade since the Fisher lab reported that epidermal eumelanin could be robustly up-regulated by topical application of forskolin, an adenylyl cyclase activator that bypassed a defective melanocortin 1 receptor (Mc1r) to promote melanin synthesis. Eumelanin induction protected fair-skinned mice from UV damage using an animal model that recapitulates many of the features of pigmented human epidermis. Through constitutive production of stem cell factor (Kit ligand) in the basal epidermis, the K14-Scf transgenic mouse retains interfollicular melanocytes in the skin and therefore accumulates melanin pigments in the epidermis...
July 5, 2017: Pigment Cell & Melanoma Research
https://www.readbyqxmd.com/read/28676423/functional-interplay-between-secreted-ligands-and-receptors-in-melanoma
#7
REVIEW
Cecilia Herraiz, Celia Jiménez-Cervantes, Berta Sánchez-Laorden, José C García-Borrón
Melanoma, the most aggressive form of skin cancer, results from the malignant transformation of melanocytes located in the basement membrane separating the epidermal and dermal skin compartments. Cutaneous melanoma is often initiated by solar ultraviolet radiation (UVR)-induced mutations. Melanocytes intimately interact with keratinocytes, which provide growth factors and melanocortin peptides acting as paracrine regulators of proliferation and differentiation. Keratinocyte-derived melanocortins activate melanocortin-1 receptor (MC1R) to protect melanocytes from the carcinogenic effect of UVR...
July 1, 2017: Seminars in Cell & Developmental Biology
https://www.readbyqxmd.com/read/28660550/clinical-and-economic-evaluation-of-repository-corticotropin-injection-a-narrative-literature-review-of-treatment-efficacy-and-healthcare-resource-utilization-for-seven-key-indications
#8
REVIEW
Michael Philbin, John Niewoehner, George J Wan
INTRODUCTION: Repository corticotropin injection (RCI; H.P. Acthar(®) Gel; Mallinckrodt Pharmaceuticals Inc., Hampton, NJ) is a highly purified, prolonged-release porcine preparation of adrenocorticotropic hormone (ACTH) analogue that is FDA-approved for treatment of 19 autoimmune and inflammatory disorders. The diverse physiological actions of RCI at the melanocortin receptors (MCRs) affect processes involved in inflammation, pigmentation, steroidogenesis, and immunomodulation. Although RCI has been approved to treat inflammatory and autoimmune diseases for more than 60 years, recent progress in understanding both MCRs and the effects of RCI in modulating immune responses has led to increased interest in RCI as a therapeutic choice...
June 28, 2017: Advances in Therapy
https://www.readbyqxmd.com/read/28651519/analysis-of-the-genetic-variation-in-mitochondrial-dna-y-chromosome-sequences-and-mc1r-sheds-light-on-the-ancestry-of-nigerian-indigenous-pigs
#9
Adeniyi C Adeola, Olufunke O Oluwole, Bukola M Oladele, Temilola O Olorungbounmi, Bamidele Boladuro, Sunday C Olaogun, Lotanna M Nneji, Oscar J Sanke, Philip M Dawuda, Ofelia G Omitogun, Laurent Frantz, Robert W Murphy, Hai-Bing Xie, Min-Sheng Peng, Ya-Ping Zhang
BACKGROUND: The history of pig populations in Africa remains controversial due to insufficient evidence from archaeological and genetic data. Previously, a Western ancestry for West African pigs was reported based on loci that are involved in the determination of coat color. We investigated the genetic diversity of Nigerian indigenous pigs (NIP) by simultaneously analyzing variation in mitochondrial DNA (mtDNA), Y-chromosome sequence and the melanocortin receptor 1 (MC1R) gene. RESULTS: Median-joining network analysis of mtDNA D-loop sequences from 201 NIP and previously characterized loci clustered NIP with populations from the West (Europe/North Africa) and East/Southeast Asia...
June 26, 2017: Genetics, Selection, Evolution: GSE
https://www.readbyqxmd.com/read/28642375/acquired-resistance-to-corticotropin-therapy-in-nephrotic-syndrome-role-of-de-novo-neutralizing-antibody
#10
Pei Wang, Yan Zhang, Yu Wang, Andrew S Brem, Zhangsuo Liu, Rujun Gong
There is increasing evidence supporting the use of corticotropin as an alternative treatment of refractory proteinuric glomerulopathies. The efficacy of short-acting corticotropin, however, remains unknown and was tested here in an adolescent with steroid-dependent nephrotic syndrome caused by minimal change disease. After developing Cushing syndrome and recently being afflicted with severe cellulitis, the patient was weaned off all immunosuppressants, including corticosteroids. This resulted in a relapse of generalized anasarca, associated with massive proteinuria and hypoalbuminemia...
June 22, 2017: Pediatrics
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
#11
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...
August 30, 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
#12
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
#13
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
#14
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/28589422/modulatory-function-of-nmda-glutamate-receptor-on-mc3-mc4-receptors-agonist-induced-hypophagia-in-neonatal-meat-type-chicken
#15
Fariba Ahmadi, Morteza Zendehdel, Vahab Babapour, Negar Panahi, Shahin Hassanpour, Mina Khodadadi
Melanocortin 3 and 4 receptors (MC3R and MC4R) are known as the main receptors for melanocortin-induced hypophagia in mammalian and poultry. Also, central glutamatergic system has mediatory role on function of the melanocortin system in some brain areas. So, the aim of the current study was to determine the role of MC3/MC4 receptors agonist on food intake and its interaction with glutamatergic in 3-h food-deprived (FD3) neonatal broilers. In experiment 1, chickens were intracerebroventricular (ICV) injected with control solution, MTII (MC3/MC4 receptors agonist; 2...
June 6, 2017: Veterinary Research Communications
https://www.readbyqxmd.com/read/28579117/key-amino-acid-residue-in-melanocortin-1-receptor-melanocyte-%C3%AE-msh-receptor-for-ligand-selectivity
#16
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
#17
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
#18
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/28552734/melanocortin-4-receptor-regulation-of-pain
#19
REVIEW
Zhi-Xiao Li, Bao-Wen Liu, Zhi-Gang He, Hong-Bing Xiang
An increasingly high occurrence of chronic pain in patients highlights the importance of fundamental research. The melanocortin-4 receptor (MC4R) regulation of pain has attracted much attention in recent years due to its high expression in the mammalian brain regions related to nociception and pain. This review is devoted to anatomic distribution of MC4R in the brain and interaction between MC4R and other pathways for pain modulation. The experimental evidence available at present had expanded our understanding of melanocortin-4 receptor regulation of pain...
May 26, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28551830/factors-responsible-for-obesity-related-hypertension
#20
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
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