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Anticatabolic properties of melanocortin-4 receptor antagonists
Current Opinion in Clinical Nutrition & Metabolic Care, 2006Health problems related to weight regulation are increasingly common in the USA and around the world. Although obesity and associated complications garner the most attention in the media, clinical problems at the opposite end of the spectrum, such as involuntary disease-associated weight loss or cachexia, are equally devastating. This review focuses on
Lisa D, Madison, Daniel L, Marks
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Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor
Bioorganic & Medicinal Chemistry Letters, 2006A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the alpha-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or beta-alanine was incorporated onto the benzylamine ...
Wanlong, Jiang +13 more
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Melanocortin-4 receptor mutations in obesity.
Advances in clinical chemistry, 2009The current alarming spread of obesity in many parts of the world is caused by a sudden environmental shift characterized by replacement of a frugal diet with low cost, energy dense food, and little requests for physical activity during work and leisure time.
SANTINI, FERRUCCIO +5 more
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Involvement of melanocortin-4 receptor in anxiety and depression
Peptides, 2005The melanocortins, which are derived from proopiomelanocortin, have a variety of physiological functions mediated membrane surface receptors. To date, five subtypes have been cloned. With the cloning of melanocortin receptors, studies with genetic models, and development of selective compounds, the physiological roles of the five melanocortin receptors
Shigeyuki, Chaki, Shigeru, Okuyama
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Melanocortin-4 Receptor (MC4R) Agonists for the Treatment of Obesity
Journal of Medicinal Chemistry, 2006AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Ravi P, Nargund +2 more
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Functional Role, Structure, and Evolution of the Melanocortin‐4 Receptor
Annals of the New York Academy of Sciences, 2003Abstract: The melanocortin (MC)‐4 receptor participates in regulating body weight homeostasis. We demonstrated early that acute blockage of the MC‐4 receptor increases food intake and relieves anorexic conditions in rats. Our recent studies show that 4‐week chronic blockage of the MC‐4 receptor leads to robust increases in food intake and development ...
HB Schioth +9 more
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2000
After cloning of the melanocyte MC1-R (1,2) and adrenocortical MC2-R (2),interest in the possibility of unique neural homologs of these receptors grew from observations of central effects of melanocortins, such as effects on learning and memory (reviewed in ref. 3) and temperature control (4).
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After cloning of the melanocyte MC1-R (1,2) and adrenocortical MC2-R (2),interest in the possibility of unique neural homologs of these receptors grew from observations of central effects of melanocortins, such as effects on learning and memory (reviewed in ref. 3) and temperature control (4).
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The genetic epidemiology of melanocortin 4 receptor variants
European Journal of Pharmacology, 2011While rare MC4R mutations are the commonest cause of monogenic forms of extreme, early-onset obesity, growing evidence shows that common MC4R variants contribute to obesity in the general population. Candidate gene studies have focussed on the V103I and I251L MC4R variants that both affect MC(4) receptor function in vitro.
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Small Molecule Ligands of the Human Melanocortin-4 Receptor
Current Topics in Medicinal Chemistry, 2007Genetic and pharmacological studies, involving both animals and humans, suggest that the central MC4 receptor plays a key role in homeostatic control, most probably via regulation of appetite and energy expenditure. This has stimulated intense research efforts in the field of drug discovery to identify MC4 receptor agonists and antagonists for the ...
Feroze, Ujjainwalla, Iyassu K, Sebhat
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Mutations in melanocortin-4 receptor: From fish to men
2022Melanocortin-4 receptor (MC4R), expressed abundantly in the hypothalamus, is a critical regulator of energy homeostasis, including both food intake and energy expenditure. Shortly after the publication in 1997 of the Mc4r knockout phenotypes in mice, including increased food intake and severe obesity, the first mutations in MC4R were reported in humans
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