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Melanocortin 4 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/28438719/chick-subcutaneous-and-abdominal-adipose-tissue-depots-respond-differently-in-lipolytic-and-adipogenic-activity-to-%C3%AE-melanocyte-stimulating-hormone-%C3%AE-msh
#2
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
#3
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
#4
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/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
#5
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/28409883/melanocortin-4-receptor-activation-attenuates-mitochondrial-dysfunction-in-skeletal-muscle-of-diabetic-rats
#6
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
#7
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
#8
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/28382155/preclinical-melanoma-imaging-with-68-ga-labeled-%C3%AE-melanocyte-stimulating-hormone-derivatives-using-pet
#9
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/28356726/searching-for-the-relationship-between-the-parameters-of-metabolic-syndrome-and-the-rs17782313-t-c-polymorphism-of-the-mc4r-gene-in-postmenopausal-women
#10
Jacek Brodowski, Małgorzata Szkup, Anna Jurczak, Sylwia Wieder-Huszla, Agnieszka Brodowska, Maria Laszczyńska, Beata Karakiewicz, Katarzyna Kęcka, Elżbieta Grochans
Metabolic syndrome (MS) is widespread in the human population, and its incidence is continuously increasing, generating serious health problems. The purpose of this study was to find the relationship between the parameters of MS and the melanocortin type 4 receptor (MC4R) gene polymorphism in postmenopausal women. The study involved 344 healthy Polish women, who had their last menstrual cycle 1 year ago or earlier. The study included blood analysis, survey, and body measurements. The mean age was 58.5±6.6 years...
2017: Clinical Interventions in Aging
https://www.readbyqxmd.com/read/28333235/ovarian-hormones-and-obesity
#11
Brigitte Leeners, Nori Geary, Philippe N Tobler, Lori Asarian
BACKGROUND: Obesity is caused by an imbalance between energy intake, i.e. eating and energy expenditure (EE). Severe obesity is more prevalent in women than men worldwide, and obesity pathophysiology and the resultant obesity-related disease risks differ in women and men. The underlying mechanisms are largely unknown. Pre-clinical and clinical research indicate that ovarian hormones may play a major role. OBJECTIVE AND RATIONALE: We systematically reviewed the clinical and pre-clinical literature on the effects of ovarian hormones on the physiology of adipose tissue (AT) and the regulation of AT mass by energy intake and EE...
March 2, 2017: Human Reproduction Update
https://www.readbyqxmd.com/read/28327432/feedback-from-arctic-charr-feed-flavour-stimulation-and-re-feeding-after-feed-deprivation-stimulate-genes-encoding-both-orexigenic-and-anorexigenic-neuropeptides
#12
Anja Striberny, Even H Jørgensen
Despite vast research attention, the knowledge about central mechanisms of appetite regulation in teleost remains inconclusive. A common strategy in studies on appetite regulating mechanisms is to measure the response to feed restriction or - deprivation, but responses vary between fish species and between experiments, and are also likely dependent on the degree of energy perturbation. The anadromous Arctic charr is an interesting model for studying appetite regulation as its feeding cycle comprises months of winter anorexia, and hyperphagia during summer...
March 19, 2017: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28324105/thyroid-hormone-dependent-epigenetic-regulation-of-melanocortin-4-receptor-levels-in-female-offspring-of-obese-rats
#13
Tzlil Tabachnik, Tatiana Kisliouk, Asaf Marco, Noam Meiri, Aron Weller
Maternal obesity is a risk factor for offspring obesity. The melanocortin 4 receptor (Mc4r) is one of the mediators of food intake and energy balance. The present study examined the epigenetic mechanisms underlying altered Mc4r levels in the hypothalamic paraventricular nucleus in the offspring of high-fat diet (HFD)-induced obese dams and sought to elucidate the role of thyroid hormones in epigenetic regulation and tagging of their nucleosome at the Mc4r promoter. Female Wistar rats were fed an HFD or standard chow from weaning through gestation and lactation...
April 1, 2017: Endocrinology
https://www.readbyqxmd.com/read/28303974/antifibrotic-effect-of-pirfenidone-in-a-mouse-model-of-human-nonalcoholic-steatohepatitis
#14
Chikara Komiya, Miyako Tanaka, Kyoichiro Tsuchiya, Noriko Shimazu, Kentaro Mori, Shunsaku Furuke, Yasutaka Miyachi, Kumiko Shiba, Shinobu Yamaguchi, Kenji Ikeda, Kozue Ochi, Kazuhiko Nakabayashi, Ken-Ichiro Hata, Michiko Itoh, Takayoshi Suganami, Yoshihiro Ogawa
Non-alcoholic steatohepatitis (NASH) is characterized by steatosis with lobular inflammation and hepatocyte injury. Pirfenidone (PFD) is an orally bioavailable pyridone derivative that has been clinically used for the treatment of idiopathic pulmonary fibrosis. However, it remains unknown whether PFD improves liver fibrosis in a mouse model with human NASH-like phenotypes. In this study, we employed melanocortin 4 receptor-deficient (MC4R-KO) mice as a mouse model with human NASH-like phenotypes to elucidate the effect and action mechanisms of PFD on the development of NASH...
March 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28284973/pharmacological-chaperones-for-the-misfolded-melanocortin-4-receptor-associated-with-human-obesity
#15
Hui Huang, Wei Wang, Ya-Xiong Tao
The melanocortin-4 receptor (MC4R) plays a vital role in regulating energy homeostasis. Mutations in the MC4R cause early-onset severe obesity. The majority of loss of function MC4R mutants are retained intracellularly, many of which are not terminally misfolded and can be stabilized and targeted to the plasma membrane by different chaperones. Some of the mutants might be functional once coaxed to the cell surface. Molecular chaperones and chemical chaperones correct the misfolding of some mutant MC4Rs. However, their therapeutic application is very limited due to their non-specific mechanism of action and, for chemical chaperone, high dosage needed to be effective...
March 8, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28274841/role-of-the-brain-melanocortins-in-blood-pressure-regulation
#16
Jussara M do Carmo, Alexandre A da Silva, Zhen Wang, Taolin Fang, Nicola Aberdein, Cecilia E Perez de Lara, John E Hall
Melanocortins play an important role in regulating blood pressure (BP) and sympathetic nervous system (SNS) activity as well as energy balance, glucose and other metabolic functions in humans and experimental animals. In experimental models of hypertension with high SNS activity, blockade of the melanocortin-4 receptor (MC4R) reduces BP despite causing marked hyperphagia and obesity. Activation of the central nervous system (CNS) pro-opiomelanocortin (POMC)-MC4R pathway appears to be an important link between obesity, SNS activation and hypertension...
March 6, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28273060/mc4r-dependent-suppression-of-appetite-by-bone-derived-lipocalin-2
#17
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 Nicholas, Wendy Chung, Lori M Zeltser, Kevin W Williams, Jeffrey E Pessin, Stavroula Kousteni
Bone has recently emerged as a pleiotropic endocrine organ that secretes at least two hormones, FGF23 and osteocalcin, which regulate kidney function and glucose homeostasis, respectively. These findings have raised the question of whether other bone-derived hormones exist and what their potential functions are. Here we identify, through molecular and genetic analyses in mice, lipocalin 2 (LCN2) as an osteoblast-enriched, secreted protein. Loss- and gain-of-function experiments in mice demonstrate that osteoblast-derived LCN2 maintains glucose homeostasis by inducing insulin secretion and improves glucose tolerance and insulin sensitivity...
March 16, 2017: Nature
https://www.readbyqxmd.com/read/28267582/melanocortin-4-receptor-ligands-modulate-energy-homeostasis-through-urocortin-1-neurons-of-the-centrally-projecting-edinger-westphal-nucleus
#18
Nóra Füredi, Ákos Nagy, Alexandra Mikó, Gergely Berta, Tamás Kozicz, Erika Pétervári, Márta Balaskó, Balázs Gaszner
The role of the urocortin 1 (Ucn1) expressing centrally projecting Edinger-Westphal (EWcp) nucleus in energy homeostasis and stress adaptation response has previously been investigated. Morphological and functional studies have proven that orexigenic and anorexigenic peptidergic afferents and receptors for endocrine messengers involved in the energy homeostasis are found in the EWcp. The central role of the hypothalamic melanocortin system in energy homeostasis is well known, however, no data have been published so far on possible crosstalk between melanocortins and EWcp-Ucn1...
March 3, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28246458/associations-between-single-nucleotide-polymorphisms-in-multiple-candidate-genes-and-body-weight-in-rabbits
#19
Karim El-Sabrout, Sarah A Aggag
AIM: In this study, we examined parts of six growth genes (growth hormone [GH], melanocortin 4 receptor [MC4R], growth hormone receptor [GHR], phosphorglycerate mutase [PGAM], myostatin [MSTN], and fibroblast growth factor [FGF]) as specific primers for two rabbit lines (V-line, Alexandria) using nucleotide sequence analysis, to investigate association between detecting single nucleotide polymorphism (SNP) of these genes and body weight (BW) at market. MATERIALS AND METHODS: Each line kits were grouped into high and low weight rabbits to identify DNA markers useful for association studies with high BW...
January 2017: Veterinary World
https://www.readbyqxmd.com/read/28243712/altered-sucrose-self-administration-following-injection-of-melanocortin-receptor-agonists-and-antagonists-into-the-ventral-tegmental-area
#20
Laranci Shanmugarajah, Anna I Dunigan, Kyle J Frantz, Aaron G Roseberry
RATIONALE AND OBJECTIVES: Alpha-melanocyte stimulating hormone (αMSH) and agouti-related protein (AgRP) are antagonistic neuropeptides that play an important role in the control of feeding and body weight through their central actions on the melanocortin-3 and melanocortin-4 receptors. Increasing evidence indicates that αMSH and AgRP can interact with the mesolimbic dopamine system to regulate feeding as well as other behaviors. For example, we have shown previously that injection of melanocortin receptor agonists and antagonists into the ventral tegmental area (VTA) alters both normal home-cage feeding and the intake of sucrose solutions, but it remains unknown whether αMSH and AgRP can also act in the VTA to affect reward-related feeding...
February 27, 2017: Psychopharmacology
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