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Molecular Characterization of Human Melanocortin-3 Receptor Ligandāˆ’Receptor Interaction

Biochemistry, 2006
Melanocortin-3 receptor (MC3R), primarily expressed in the hypothalamus, plays an important role in the regulation of energy homeostasis. MC3R-deficient (MC3R(-)(/)(-)) mice demonstrate increased fat mass, higher feeding efficiency, hyperleptinaemia, and mild hyperinsulinism.
Min, Chen   +6 more
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Rattus norvegicus melanocortin 3 receptor: A corrected sequence

Peptides, 2005
Examination of the Rattus norvegicus genome reveals differences in the melanocortin 3 receptor (MC3R) compared with the published sequence (accession X70667). To clarify these differences, we used RT-PCR to clone MC3R from Sprague Dawley rats. These efforts revealed a sequence for the rat MC3R consistent with that predicted by the rat genome, but ...
Derek, Daniels   +5 more
openaire   +2 more sources

The Role of the Melanocortin‐3 Receptor in Cachexia

Annals of the New York Academy of Sciences, 2003
Abstract: Cachexia refers to a synergistic combination of a dramatic decrease in appetite and an increase in metabolism of fat and lean body mass. This combination is found in a number of chronic diseases and is an important determinant of mortality. In this paper, we provide evidence that in both acute and chronic disease models, blockade of the MC4 ...
Daniel L, Marks, Roger D, Cone
openaire   +2 more sources

Melanocortin-3 receptor activates MAP kinase via PI3 kinase

Regulatory Peptides, 2007
HEK 293 cells stably expressing human melanocortin-3 receptor (MC3R) were exposed to melanocortin receptor agonist, NDP-MSH (10(-)(10)-10(-)(6) M). ERK1/2 was phosphorylated in a dose-dependent manner with an EC(50) of 3.3+/-1.5 x 10(-)(9) M, similar to the IC(50) of NDP-MSH binding to the MC3R.
Biaoxin, Chai   +4 more
openaire   +2 more sources

Melanocortin 3 receptor gene and melanocortin 4 receptor gene mutations: the Asian Perspective

Diabetes/Metabolism Research and Reviews, 2012
SummaryMelanocortin 4 receptor (MC4R) deficiency resulting from disruption of one or both MC4R alleles represents the commonest monogenic form of human obesity to date. Human MC4R deficiency was reported to affect 4 and 5.8% of severely obese French and British populations respectively.
openaire   +2 more sources

N-Branched Tricyclic Guanidines as Novel Melanocortin-3 Receptor Agonists and Melanocortin-4 Receptor Antagonists

Journal of Medicinal Chemistry
The melanocortin receptors are a class of centrally and peripherally expressed G protein-coupled receptors, of which the MC3R and MC4R subtypes are implicated in the regulation of appetite and energy homeostasis and can serve as potential therapeutic targets for disorders such as obesity and cachexia.
Nicholas A. Weirath   +11 more
openaire   +2 more sources

Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptors.

The Journal of Pharmacology and Experimental Therapeutics, 1995
The melanocortins are peptide products of proopiomelanocortin post-translational processing that, among other functions, are thought to influence cognition. Recently, we isolated genes encoding two human melanocortin receptors, the melanocortin-3 receptor (hMC3R) and the melanocortin-4 receptor (hMC4R), which are expressed primarily in brain.
H, Miwa   +4 more
openaire   +2 more sources

Functional characterization of the mouse melanocortin 3 receptor gene promoter

Gene, 2015
Melanocortin receptor 3 (MC3R) is expressed in the hypothalamus and pituitary in humans and rodents, and is involved in the control of feeding, energy metabolism, and pituitary function. In the mouse pituitary, MC3R is detected in mammotrophs. This study aimed to clarify the regulatory mechanism for Mc3r expression in the mouse pituitary.
Keisuke, Okutsu   +9 more
openaire   +2 more sources

Pharmacology of the giant panda (Ailuropoda melanoleuca) melanocortin-3 receptor

General and Comparative Endocrinology, 2019
The melanocortin-3 receptor (MC3R) is a member of the G protein-coupled receptor superfamily that plays a critical role in controlling energy balance and metabolism. Although pharmacological characterization of MC3R has been reported previously in several other species, there is no report on the MC3R from giant panda (Ailuropoda melanoleuca).
Hai-Jie Zhang   +4 more
openaire   +2 more sources

Mutations in Melanocortin-3 Receptor Gene and Human Obesity

2016
The prevalence of obesity calls for novel therapeutic targets. The melanocortin-3 receptor (MC3R) has been increasingly recognized as an important regulator of energy homeostasis and MC3R has been intensively analyzed in molecular genetic studies for obesity-related traits.
Z, Yang, Y-X, Tao
openaire   +2 more sources

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