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Propionylpiperazines as human melanocortin-4 receptor ligands
Bioorganic and Medicinal Chemistry Letters, 2006A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain penetration in mice.
Caroline W Chen +2 more
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Melanocortin 4 receptor mutations become common
Cell Metabolism, 2021In a new paper, Wade et al. (2021) analyzed the frequency of MC4R loss-of-function (LoF) mutations in a population-based Avon Longitudinal Study of Parents and Children. The frequency was 1 in 337 and the authors showed that MC4R LoF variants significantly correlated with increased body weight and fat mass in children and adults (cumulating in ...
Peter, Kühnen +2 more
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Characterisation of the Melanocortin 4 Receptor by Radioligand Binding
Pharmacology & Toxicology, 1996Abstract: The DNA encoding the human melanocortin 4 receptor was expressed in COS (CV‐1 origin, SV 40) cells and its radioligand binding properties was tested by using the [125I][Nle4, D‐Phe7]α‐melanocyte stimulating hormone (MSH). The radioligand was found to bind to a single saturable site with a Kd of 3.84±0.57 nmol/1 in the MC4 receptor expressing
H B, Schiöth +2 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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Melanocortin - 4 Receptor Agonists for the Treatment of Obesity
Current Topics in Medicinal Chemistry, 2007The melanocortin family of receptors (MC 1-5R) and their endogenous peptide ligands (alpha, beta, gamma- MSH and ACTH) have been implicated in the control of a wide variety of behavioral and physiological functions including the homeostatic control of food intake and body weight.
Paul J, Emmerson +3 more
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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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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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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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General and Comparative Endocrinology, 2018
Melanocortin 4 receptor (MC4R), which is a member of the G protein-coupled receptor (GPCR) family, mediates regulation of energy homeostasis upon the binding of α-melanocyte-stimulating hormone (α-MSH) in the central nervous system (CNS). Melanocortin 2 receptor accessory protein 2 (MRAP2) modulates the function of MC4R.
Makoto, Habara +7 more
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Melanocortin 4 receptor (MC4R), which is a member of the G protein-coupled receptor (GPCR) family, mediates regulation of energy homeostasis upon the binding of α-melanocyte-stimulating hormone (α-MSH) in the central nervous system (CNS). Melanocortin 2 receptor accessory protein 2 (MRAP2) modulates the function of MC4R.
Makoto, Habara +7 more
openaire +2 more sources