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Glutamatergic melanocortin‐4 receptor neurons regulate body weight
The FASEB Journal, 2023Abstract The locus coeruleus (LC), enriched in vesicular glutamate transporter 2 (VGlut2) neurons, is a potential homeostasis‐regulating hub. However, the identity of melanocortin‐4 receptor (MC4R) neurons in the paraventricular nucleus (PVN) of the hypothalamus, PVN VGlut2::MC4R
Haodong Liu +12 more
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Propionylpiperazines as human melanocortin-4 receptor ligands
Bioorganic & 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 +13 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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Melanocortin-4 Receptor Gene Polymorphisms in Obese Patients
Biochemical Genetics, 2009Obesity is a complex disease caused by both genetics and environmental factors. Melanocortin-4 receptor (MC4R) (MIM 155541) gene polymorphisms were reported to be the cause of monogenic obesity in humans. We studied three polymorphisms (Val50Met, Val103Ile, and Ser58Cys) and a mutation (Asn274Ser) of the MC4R gene in 203 obese patients and in 110 ...
YETKİN, İLHAN +8 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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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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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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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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Melanocortin 4 receptors interact with antimicrobial frog peptide analogues
Biochemical and Biophysical Research Communications, 2006We have developed fluorescence polarization (FP) assays of human melanocortin 4 receptor (MC4R) in 384-well microtiter plates using TAMRA-NDP-MSH as a tracer. The rank order of potency of agonists and antagonists agrees well relative to the published assays: SHU9119>MTII>NDP alphaMSH>alphaMSH.
Ernest U, Do +10 more
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Melanocortin-4 Receptor Gene and Complications after Gastric Banding
Obesity Surgery, 2006Mutations of the melanocortin-4 receptor (MC4R) gene are associated with up to 5.8% of monogenetic causes of obesity. Correlations between defects in MC4R and complications after laparoscopic adjustable gastric banding (LAGB) have recently been reported.
Ralph, Peterli +4 more
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