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melanocortin receptor

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https://www.readbyqxmd.com/read/28453292/discovery-of-mixed-pharmacology-melanocortin-3-agonists-and-melanocortin-4-receptor-tetrapeptide-antagonist-compounds-tacos-based-on-the-sequence-ac-xaa-1-arg-pi-dphe-xaa-4-nh2
#1
Skye R Doering, Katie T Freeman, Sathya M Schnell, Erica M Haslach, Marvin Louie Servanez Dirain, Ginamari Ginamarie Debevec, Phaedra Geer, Radleigh G Santos, Marc A Giulianotti, Clemencia Pinilla, Jon R Appel, Robert C Speth, Richard A Houghten, Carrie Haskell-Luevano
The centrally expressed melanocortin-3 and -4 receptors (MC3R/MC4R) have been studied as possible targets for weight management therapies, with a preponderance of studies focusing on the MC4R. Herein, a novel tetrapeptide scaffold [Ac-Xaa1-Arg-(pI)DPhe-Xaa4-NH2] is reported. The scaffold was derived from results obtained from a MC3R mixture-based positional scanning campaign. From these results, a set of 48 tetrapeptides were designed and pharmacologically characterized at the mouse melanocortin-1, -3, -4, and -5 receptors...
April 28, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28442450/implementing-an-internet-delivered-skin-cancer-genetic-testing-intervention-to-improve-sun-protection-behavior-in-a-diverse-population-protocol-for-a-randomized-controlled-trial
#2
Jennifer L Hay, Marianne Berwick, Kate Zielaskowski, Kirsten Am White, Vivian M Rodríguez, Erika Robers, Dolores D Guest, Andrew Sussman, Yvonne Talamantes, Matthew R Schwartz, Jennie Greb, Jessica Bigney, Kimberly A Kaphingst, Keith Hunley, David B Buller
BACKGROUND: Limited translational genomic research currently exists to guide the availability, comprehension, and appropriate use of personalized genomics in diverse general population subgroups. Melanoma skin cancers are preventable, curable, common in the general population, and disproportionately increasing in Hispanics. OBJECTIVE: Variants in the melanocortin-1 receptor (MC1R) gene are present in approximately 50% of the population, are major factors in determining sun sensitivity, and confer a 2-to-3-fold increase in melanoma risk in the general population, even in populations with darker skin...
April 25, 2017: JMIR Research Protocols
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
#3
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...
April 21, 2017: Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology
https://www.readbyqxmd.com/read/28434791/neuronal-cells-derived-from-human-induced-pluripotent-stem-cells-as-a-functional-tool-of-melanocortin-system
#4
Nobuko Yamada-Goto, Yukari Ochi, Goro Katsuura, Yui Yamashita, Ken Ebihara, Michio Noguchi, Junji Fujikura, Daisuke Taura, Masakatsu Sone, Kiminori Hosoda, Paul E Gottschall, Kazuwa Nakao
BACKGROUND: The preparation of human neurons derived from human induced pluripotent stem (iPS) cells can serve as a potential tool for evaluating the physiological and pathophysiological properties of human neurons and for drug development. METHODS: In the present study, the functional activity in neuronal cells differentiated from human iPS cells was observed. RESULTS: The differentiated cells expressed mRNAs for classical neuronal markers (microtubule-associated protein 2, β-tubulin III, calbindin 1, synaptophysin and postsynaptic density protein 95) and for subunits of various excitatory and inhibitory transmitters (NR1, NR2A, NR2B, GABAA α1)...
April 7, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28433713/biased-signaling-at-neural-melanocortin-receptors-in-regulation-of-energy-homeostasis
#5
Li-Kun Yang, Ya-Xiong Tao
The global prevalence of obesity highlights the importance of understanding on regulation of energy homeostasis. The central melanocortin system is an important intersection connecting the neural pathways controlling satiety and energy expenditure to regulate energy homeostasis by sensing and integrating the signals of external stimuli. In this system, neural melanocortin receptors, melanocortin-3 and -4 receptors (MC3R and MC4R), play crucial roles in the regulation of energy homeostasis. Recently, multiple intracellular signaling pathways and biased signaling at neural MCRs have been discovered, providing new insights into neural MCR signaling...
April 19, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28429261/localization-of-the-dopamine-receptors-of-types-1-and-2-on-the-bodies-of-pomc-expressing-neurons-of-the-arcuate-nucleus-of-the-hypothalamus-in-mice-and-rats
#6
I V Romanova, A L Mikhrina, A O Shpakov
Using immunofluorescent techniques, we have demonstrated the presence of two main types of dopamine receptors, D1 and D2, on the bodies of neurons of the arcuate nucleus of the hypothalamus expressing the precursor of peptides of the melanocortin family proopiomelanocortin in C57Bl/6J mice and Wistar rats. These data show close functional relationship between the dopamine and melanocortin systems of the brain and involvement of dopamine in the control of synthesis and secretion of peptides of the melanocortin family...
January 2017: Doklady Biological Sciences: Proceedings of the Academy of Sciences of the USSR, Biological Sciences Sections
https://www.readbyqxmd.com/read/28426141/melanocortin-2-3-and-4-receptor-gene-expressions-are-downregulated-in-cd8-t-cytotoxic-lymphocytes-and-cd19-b-lymphocytes-in-rheumatoid-arthritis-responding-to-tnf%C3%AE-inhibition
#7
Marlene Andersen, Ivan Nagaev, Michael Kruse Meyer, Olga Nagaeva, Jarl Wikberg, Lucia Mincheva-Nilsson, Grethe Neumann Andersen
Melanocortin signaling in leukocyte subsets elicits anti-inflammatory and immune tolerance inducing effects in animal experimental inflammation. In man, however, the effects of melanocortin signaling in inflammatory conditions have scarcely been examined. We explored the differential reactions of melanocortin 1-5 receptor (MC1-5R) gene expressions in pathogenetic leukocyte subsets in rheumatoid arthritis (RA) to treatment with TNFα inhibitor adalimumab. Seven patients with active RA donated blood at start and at three months treatment...
April 20, 2017: Scandinavian Journal of Immunology
https://www.readbyqxmd.com/read/28424580/the-role-of-microrna-in-the-modulation-of-the-melanocortinergic-system
#8
REVIEW
Adel Derghal, Mehdi Djelloul, Jérôme Trouslard, Lourdes Mounien
The central control of energy balance involves a highly regulated neuronal network within the hypothalamus and the dorsal vagal complex. In these structures, pro-opiomelanocortin (POMC) neurons are known to reduce meal size and to increase energy expenditure. In addition, leptin, a peripheral signal that relays information regarding body fat content, modulates the activity of melanocortin pathway neurons including POMC-, Agouti-related peptide (AgRP)/Neuropeptide Y (NPY)-, melanocortin receptors (MC3R and MC4R)-expressing neurons...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28409883/melanocortin-4-receptor-activation-attenuates-mitochondrial-dysfunction-in-skeletal-muscle-of-diabetic-rats
#9
Hao-Hao Zhang, Jiao Liu, Gui-Jun Qin, Xia-Lian Li, Pei-Jie Du, Xiao Hao, Tian-Tian Tian, Jing- Wu, Meng- Yun, Yan-Hui Bai
Backgroud: A previous study has confirmed that the central melanocortin system was able to mediate skeletal muscle AMP-activated protein kinase (AMPK) activation in mice fed a high-fat diet, while activation of the AMPK signaling pathway significantly induced mitochondrial biogenesis. Our hypothesis was that melanocortin 4 receptor (MC4R) was involved in the development of skeletal muscle injury in diabetic rats. METHODS: In this study, we treated diabetic rats intracerebroventricularly with MC4R agonist R027-3225 or antagonist SHU9119, respectively...
April 14, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28403939/melanocortin-4-receptor-is-not-required-for-estrogenic-regulations-on-energy-homeostasis-and-reproduction
#10
Pingwen Xu, Liangru Zhu, Kenji Saito, Yongjie Yang, Chunmei Wang, Yanlin He, Xiaofeng Yan, Ilirjana Hyseni, Qingchun Tong, Yong Xu
BACKGROUND: Brain estrogen receptor-α (ERα) is essential for estrogenic regulation of energy homeostasis and reproduction. We previously showed that ERα expressed by pro-opiomelanocortin (POMC) neurons mediates estrogen's effects on food intake, body weight, negative regulation of hypothalamic-pituitary-gonadal axis (HPG axis) and fertility. RESULTS AND CONCLUSIONS: We report here that global deletion of a key downstream receptor for POMC peptide, the melanocortin 4 receptor (MC4R), did not affect normal negative feedback regulation of estrogen on the HPG axis, estrous cyclicity and female fertility...
May 2017: Metabolism: Clinical and Experimental
https://www.readbyqxmd.com/read/28396685/associations-of-two-obesity-related-single-nucleotide-polymorphisms-with-adiponectin-in-chinese-children
#11
Lijun Wu, Liwang Gao, Xiaoyuan Zhao, Meixian Zhang, Jianxin Wu, Jie Mi
Purpose. Genome-wide association studies have found two obesity-related single-nucleotide polymorphisms (SNPs), rs17782313 near the melanocortin-4 receptor (MC4R) gene and rs6265 near the brain-derived neurotrophic factor (BDNF) gene, but the associations of both SNPs with other obesity-related traits are not fully described, especially in children. The aim of the present study is to investigate the associations between the SNPs and adiponectin that has a regulatory role in glucose and lipid metabolism. Methods...
2017: International Journal of Endocrinology
https://www.readbyqxmd.com/read/28396017/cell-surface-targeting-of-the-melanocortin-5-receptor-mc5r-requires-serine-rich-terminal-motifs
#12
A R Rodrigues, D Sousa, H Almeida, A M Gouveia
The Melanocortin 5 Receptor (MC5R) is a cell surface receptor that belongs to the class of G-protein coupled receptors (GPCRs), which comprises an intracellular carboxylic domain, seven transmembrane helices and an extracellular amino terminal. Over the last few years, MC5R has been implicated in the regulation of lipid metabolism in exocrine glands, muscle and even in adipose tissue and its function is quite dependent on its correct cell membrane targeting. In this context, the purpose of this work was to study the role of MC5R N-terminus in the receptor trafficking from the endoplasmic reticulum (ER) through the Golgi complex to the plasma membrane...
April 8, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28388573/amsh-prevents-ros-induced-apoptosis-by-inhibiting-foxo1-mtorc2-in-mice-adipose-tissue
#13
Weina Cao, Meihang Li, Tianjiao Wu, Fei Feng, Tongying Feng, Yang Xu, Chao Sun
Alpha-melanocyte stimulating hormone (αMSH) is an important adenohypophysis polypeptide hormone that regulates body metabolic status. To date, it is well known that the disorder of hypothalamic αMSH secretion is related to many metabolic diseases, such as obesity and type II diabetes. However, the underlying mechanisms are poorly understood. In our study, we focused on the reactive oxygen species (ROS)-induced adipocyte apoptosis and tried to unveil the role of αMSH in this process and the signal pathway which αMSH acts through...
March 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/28384517/biomarker-response-and-hypothalamus-pituitary-interrenal-axis-functioning-in-arctic-charr-from-bj%C3%A3-rn%C3%A3-ya-74%C3%A2-30-%C3%A2-n-norway-with-high-levels-of-organohalogenated-compounds
#14
Even H Jørgensen, Alec G Maule, Anita Evenset, Guttorm Christensen, Jenny Bytningsvik, Marianne Frantzen, Vladimir Nikiforov, Erin Faught, Mathilakath M Vijayan
The populations of Arctic charr (Salvelinus alpinus) residing in Lake Ellasjøen at Bjørnøya Island in the Norwegian Arctic (74° 30'N, 19° 00'E) possess substantially higher levels of organohalogenated compounds (strongly dominated by polychlorinated biphenyls, PCBs) than conspecifics residing in other, proximate lakes on the island. In the present study we sampled large (<400g), immature charr from Lake Ellasjøen (high PCB levels) and Lake Laksvatn (reference lake, low PCB levels) by hook and line for an immediate blood sampling, and blood and tissue sampling after a 1h confinement stressor...
March 20, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28382155/preclinical-melanoma-imaging-with-68-ga-labeled-%C3%AE-melanocyte-stimulating-hormone-derivatives-using-pet
#15
Chengcheng Zhang, Zhengxing Zhang, Kuo-Shyan Lin, Jinhe Pan, Iulia Dude, Navjit Hundal-Jabal, Nadine Colpo, François Bénard
It is estimated that melanoma accounted for 76,380 new cases and 10,130 deaths in the United States in 2016. The melanocortin 1 receptor (MC1R) is highly expressed in the vast majority of melanomas, which makes it an attractive target for molecular imaging and radionuclide therapy. Lactam bridge-cyclized α-melanocyte-stimulating hormone (Ac-Nle(4)-cyclo[Asp(5)-His-D-Phe(7)-Arg-Trp-Lys(10)]-NH2, or Nle-CycMSHhex) analogues have been successfully developed and studied for MC1R-targeted imaging, predominantly with single-photon emission computed tomography (SPECT)...
2017: Theranostics
https://www.readbyqxmd.com/read/28378841/%C3%AE-msh-and-melanocortin-receptors-at-early-ontogeny-in-european-sea-bass-dicentrarchus-labrax-l
#16
A Tsalafouta, M Gorissen, T N M Pelgrim, N Papandroulakis, G Flik, M Pavlidis
Temporal patterns of whole-body α-MSH concentrations and of transcripts of melanocortin receptors during early development as well as the endocrine response (α-MSH, cortisol, MCR mRNAs) to stress at the end of the larval period were characterized in Dicentrarchus labrax. Immunohistochemistry showed α-MSH positive cells in the pituitary pars intermedia in all stages examined. As development proceeds, α-MSH content gradually increases; mRNA levels of mc2r and mc4r remain low until first feeding where peak values are observed...
April 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28363699/bench-top-to-clinical-therapies-a-review-of-melanocortin-ligands-from-1954-to-2016
#17
REVIEW
Mark D Ericson, Cody J Lensing, Katlyn A Fleming, Katherine N Schlasner, Skye R Doering, Carrie Haskell-Luevano
The discovery of the endogenous melanocortin agonists in the 1950s have resulted in sixty years of melanocortin ligand research. Early efforts involved truncations or select modifications of the naturally occurring agonists leading to the development of many potent and selective ligands. With the identification and cloning of the five known melanocortin receptors, many ligands were improved upon through bench-top in vitro assays. Optimization of select properties resulted in ligands adopted as clinical candidates...
March 29, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28363697/polymorphisms-and-mutations-in-the-melanocortin-3-receptor-and-their-relation-to-human-obesity
#18
REVIEW
Andrew P Demidowich, Joo Yun Jun, Jack A Yanovski
Inactivating mutations in the melanocortin 3 receptor (Mc3r) have been described as causing obesity in mice, but the physiologic effects of MC3R mutations in humans have been less clear. Here we review the MC3R polymorphisms and mutations identified in humans, and the in vitro, murine, and human cohort studies examining their putative effects. Some, but not all, studies suggest that the common human MC3R variant T6K+V81I, as well as several other rare, function-altering mutations, are associated with greater adiposity and hyperleptinemia with altered energy partitioning...
March 28, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28361271/the-development-of-translational-biomarkers-as-a-tool-for-improving-the-understanding-diagnosis-and-treatment-of-chronic-neuropathic-pain
#19
David A Buckley, Elaine M Jennings, Nikita N Burke, Michelle Roche, Veronica McInerney, Jonathan D Wren, David P Finn, Patrick C McHugh
Chronic neuropathic pain (CNP) is one of the most significant unmet clinical needs in modern medicine. Alongside the lack of effective treatments, there is a great deficit in the availability of objective diagnostic methods to reliably facilitate an accurate diagnosis. We therefore aimed to determine the feasibility of a simple diagnostic test by analysing differentially expressed genes in the blood of patients diagnosed with CNP of the lower back and compared to healthy human controls. Refinement of microarray expression data was performed using correlation analysis with 3900 human 2-colour microarray experiments...
March 30, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28360832/a-life-without-hunger-the-ups-and-downs-to-modulating-melanocortin-3-receptor-signaling
#20
REVIEW
Andrew A Butler, Clemence Girardet, Maria Mavrikaki, James L Trevaskis, Heather Macarthur, Daniel L Marks, Susan A Farr
Melanocortin neurons conserve body mass in hyper- or hypo-caloric conditions by conveying signals from nutrient sensors into areas of the brain governing appetite and metabolism. In mice, melanocortin-3 receptor (MC3R) deletion alters nutrient partitioning independently of hyperphagia, promoting accumulation of fat over muscle mass. Enhanced rhythms in insulin and insulin-responsive metabolic genes during hypocaloric feeding suggest partial insulin resistance and enhanced lipogenesis. However, exactly where and how MC3Rs affect metabolic control to alter nutrient partitioning is not known...
2017: Frontiers in Neuroscience
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