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https://www.readbyqxmd.com/read/28813605/structure-activity-relationship-studies-on-a-macrocyclic-agouti-related-protein-agrp-scaffold-reveal-agouti-signaling-protein-asp-residue-substitutions-maintain-melanocortin-4-receptor-antagonist-potency-and-result-in-inverse-agonist-pharmacology-at-the-melanocortin
#1
Mark D Ericson, Katie T Freeman, Sathya M Schnell, Katlyn A Fleming, Carrie Haskell-Luevano
The melanocortin system consists of five reported receptors, agonists from the proopiomelanocortin gene transcript, and two antagonists, agouti-signaling protein (ASP) and agouti-related protein (AGRP). For both ASP and AGRP, the hypothesized Arg-Phe-Phe pharmacophores are on exposed β-hairpin loops. In this study, the Asn and Ala positions of a reported AGRP macrocyclic scaffold (c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro]) were explored with 14-compound and 8-compound libraries, respectively, to generate more potent, selective melanocortin receptor antagonists...
August 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28799434/metabolic-biomarkers-and-gallstone-disease-a-population-based-study
#2
Daniel Mønsted Shabanzadeh, Tea Skaaby, Lars Tue Sørensen, Jesper Eugen-Olsen, Torben Jørgensen
OBJECTIVES: The objectives for this study were to examine the associations between metabolic biomarkers of obesity including insulin resistance, vascular dysfunction, systemic inflammation, genetic susceptibility and ultrasound proven gallstone disease or cholecystectomy in a population-based cross-sectional study. MATERIAL AND METHODS: A total of 2650 participants were included, of whom 422 had gallstone disease. Associations between selected metabolic biomarkers and gallstone disease were estimated by multivariable logistic regression models and expressed as odds ratio (OR) and 95% confidence interval (CI)...
August 11, 2017: Scandinavian Journal of Gastroenterology
https://www.readbyqxmd.com/read/28791594/melanocortin-receptor-4-and-glioblastoma-cells-effects-of-the-selective-antagonist-ml00253764-alone-and-in-combination-with-temozolomide-in-vitro-and-in-vivo
#3
Francesca Vaglini, Carla Pardini, Teresa Di Desidero, Paola Orlandi, Francesco Pasqualetti, Alessandra Ottani, Simone Pacini, Daniela Giuliani, Salvatore Guarini, Guido Bocci
Currently, no description of melanocortin receptor-4 (MC4R) expression or activity is available in human cancer cells, including glioblastoma (GBM). The aim of this study is to evaluate the presence of MC4Rs in GBM cells and the selective inhibition of their activity through the MC4R antagonist ML00253764 alone and in association with temozolomide in vitro and in vivo. MC4R genotyping and gene expression were performed on human GBM cells (U-87 and U-118) with real-time PCR. MC4R western blotting, immunohistochemistry, and immunofluorescence were obtained in both cell lines and in human tissues...
August 8, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28782535/alpha-melanocyte-stimulating-hormone-induced-anorexia-in-japanese-quail-coturnix-japonica-likely-involves-the-ventromedial-hypothalamus-and-paraventricular-nucleus-of-the-hypothalamus
#4
Taylor Lear, Lingbin Liu, Madison O'Donnell, Betty R McConn, D Michael Denbow, Mark A Cline, Elizabeth R Gilbert
Alpha-melanocyte stimulating hormone (α-MSH) reduces food intake in birds and mammals. The objective of this experiment was to determine effects of α-MSH on food and water intake, and hypothalamic c-Fos immunoreactivity and appetite-associated factor mRNA in Japanese quail (Coturnix japonica), a species that has not undergone the same artificial selection for growth-related traits as the chicken. At 7days post-hatch, 3-h-fasted quail were intracerebroventricularly (ICV) injected into the lateral ventricle with 0 (vehicle), 0...
August 4, 2017: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28755272/polymorphism-and-methylation-of-the-mc4r-gene-in-obese-and-non-obese-dogs
#5
Monika Mankowska, Joanna Nowacka-Woszuk, Aneta Graczyk, Paulina Ciazynska, Monika Stachowiak, Marek Switonski
The dog is considered to be a useful biomedical model for human diseases and disorders, including obesity. One of the numerous genes associated with human polygenic obesity is MC4R, encoding the melanocortin 4 receptor. The aim of our study was to analyze polymorphisms and methylation of the canine MC4R in relation to adiposity. Altogether 270 dogs representing four breeds predisposed to obesity: Labrador Retriever (n = 187), Golden Retriever (n = 38), Beagle (n = 28) and Cocker Spaniel (n = 17), were studied...
July 28, 2017: Molecular Biology Reports
https://www.readbyqxmd.com/read/28739551/the-description-of-a-new-case-with-proopiomelanocortin-pomc-deficiency-an-increasingly-important-diagnosis-to-make
#6
Semra Çetinkaya, Tülay Güran, Erdal Kurnaz, Melikşah Keskin, Elif Sağsak, Senay Savaş Erdeve, Jenifer P Suntharalingham, Federica Buonocore, John Achermann, Zehra Aycan
International surveillance data suggests a worldwide epidemic of pediatric obesity regardless of geographic, socioeconomic, racial and ethnic factors. Reversing this epidemic of pediatric obesity will require recognition and understanding of the pathophysiology of the condition to enable us to develop novel therapies as well as taking measures to shift social attitudes and public policies at a global level. Proopiomelanocortin (POMC) deficiency is a rare monogenic disorder of early-onset obesity, which has increased our insight into the important role of the leptin-melanocortin pathway in energy balance...
July 24, 2017: Journal of Clinical Research in Pediatric Endocrinology
https://www.readbyqxmd.com/read/28738459/-gene-gene-interaction-on-central-obesity-in-school-aged-children-in-china
#7
L W Fu, M X Zhang, L J Wu, L W Gao, J Mi
Objective: To investigate possible effect of 6 obesity-associated SNPs in contribution to central obesity and examine whether there is an interaction in the 6 SNPs in the cause of central obesity in school-aged children in China. Methods: A total of 3 502 school-aged children who were included in Beijing Child and Adolescent Metabolic Syndrome (BCAMS) Study were selected, and based on the age and sex specific waist circumference (WC) standards in the BCAMS study, 1 196 central obese cases and 2 306 controls were identified...
July 10, 2017: Zhonghua Liu Xing Bing Xue za Zhi, Zhonghua Liuxingbingxue Zazhi
https://www.readbyqxmd.com/read/28727208/differential-expression-of-appetite-regulating-genes-in-avian-models-of-anorexia-and-obesity
#8
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
#9
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/28699792/novel-approaches-to-the-design-of-bioavailable-melanotropins
#10
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/28636007/analysis-of-association-of-gene-variants-with-obesity-traits-in-new-zealand-european-children-at-6-years-of-age
#11
Mohanraj Krishnan, John M D Thompson, Edwin A Mitchell, Rinki Murphy, Lesley M E McCowan, Andrew N Shelling, G On Behalf Of The Children Of Scope Study Group
Childhood obesity is a public health problem, which is associated with a long-term increased risk of cardiovascular disease and premature mortality. Several gene variants have previously been identified that have provided novel insights into biological factors that contribute to the development of obesity. As obesity tracks through childhood into adulthood, identification of the genetic factors for obesity in early life is important. The objective of this study was to identify putative associations between genetic variants and obesity traits in children at 6 years of age...
July 25, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28617454/corrigendum-mc4r-dependent-suppression-of-appetite-by-bone-derived-lipocalin-2
#12
Ioanna Mosialou, Steven Shikhel, Jian-Min Liu, Antonio Maurizi, Na Luo, Zhenyan He, Yiru Huang, Haihong Zong, Richard A Friedman, Jonathan Barasch, Patricia Lanzano, Liyong Deng, Rudolph L Leibel, Mishaela Rubin, Thomas Nickolas, Wendy Chung, Lori M Zeltser, Kevin W Williams, Jeffrey E Pessin, Stavroula Kousteni
This corrects the article DOI: 10.1038/nature21697.
June 14, 2017: Nature
https://www.readbyqxmd.com/read/28593922/copy-number-variations-in-classical-obesity-candidate-genes-are-not-frequently-associated-with-severe-early-onset-obesity-in-children
#13
Jan Windholz, Peter Kovacs, Marina Schlicke, Christin Franke, Anubha Mahajan, Andrew P Morris, Johannes R Lemke, Jürgen Klammt, Wieland Kiess, Torsten Schöneberg, Roland Pfäffle, Antje Körner
BACKGROUND: Obesity is genetically heterogeneous and highly heritable, although polymorphisms explain the phenotype in only a small proportion of obese children. We investigated the presence of copy number variations (CNVs) in "classical" genes known to be associated with (monogenic) early-onset obesity in children. METHODS: In 194 obese Caucasian children selected for early-onset and severe obesity from our obesity cohort we screened for deletions and/or duplications by multiplex ligation-dependent probe amplification reaction (MLPA)...
May 1, 2017: Journal of Pediatric Endocrinology & Metabolism: JPEM
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
#14
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/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/28579220/the-polymorphism-rs17782313-near-mc4r-gene-is-related-with-anthropometric-changes-in-women-submitted-to-bariatric-surgery-over-60-months
#16
Cristina Maria Mendes Resende, Danielle Fernandes Durso, Karina Braga Gomes Borges, Rafaela Messias Pereira, Gisele Kuhlmann Duarte Rodrigues, Kathryna Fontana Rodrigues, José Luiz Padilha Silva, Erica Castilho Rodrigues, Gloria Regina Franco, Jacqueline Isaura Alvarez-Leite
OBJECTIVE: Evaluate whether the polymorphism rs17782313 near MC4R gene influences long-term outcomes after bariatric surgery. METHODS: The rs16782313 polymorphism was genotyped in 217 individuals undergoing bariatric surgery and analyzed in detail in 141 women. Data for comorbidities, BMI, excess weight loss (EWL), and body composition were obtained before and during 60 months after surgery. RESULTS: The risk allele was found in 65 (47%) of the 141 women...
May 22, 2017: Clinical Nutrition: Official Journal of the European Society of Parenteral and Enteral Nutrition
https://www.readbyqxmd.com/read/28579117/key-amino-acid-residue-in-melanocortin-1-receptor-melanocyte-%C3%AE-msh-receptor-for-ligand-selectivity
#17
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...
October 15, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28576837/hypothalamic-inflammation-in-human-obesity-is-mediated-by-environmental-and-genetic-factors
#18
Carina Kreutzer, Sönke Peters, Dominik M Schulte, Daniela Fangmann, Kathrin Türk, Stephan Wolff, Thilo van Eimeren, Markus Ahrens, Jan Beckmann, Clemens Schafmayer, Thomas Becker, Tina Kerby, Axel Rohr, Christian Riedel, Femke-Anouska Heinsen, Frauke Degenhardt, Andre Franke, Philip Rosenstiel, Nana Zubek, Christian Henning, Sandra Freitag-Wolf, Astrid Dempfle, Aristea Psilopanagioti, Helen Petrou-Papadaki, Lennart Lenk, Olav Jansen, Stefan Schreiber, Matthias Laudes
Obesity is associated with hypothalamic inflammation (HI) in animal models. In the present study we examined the mediobasal hypothalamus (MBH) of 57 obese human subjects and 54 age- and sex- matched non-obese controls by MRI and analyzed the T2-hyperintensity as a measure of HI. Obese subjects exhibited T2-hyperintensity in the left but not the right MBH which was strongly associated with systemic low-grade inflammation. MRI-spectroscopy revealed the number of neurons in the left hypothalamic region to be similar in obese versus control subjects suggesting functional but not structural impairment due to the inflammatory process...
June 2, 2017: Diabetes
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
#19
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
#20
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
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