Orange-spotted grouper melanocortin-4 receptor: modulation of signaling by MRAP2.
Sign Up to like & getrecommendations! Published in 2019 at "General and comparative endocrinology"
DOI: 10.1016/j.ygcen.2019.113234
Abstract: Melanocortin-4 receptor (MC4R) and melanocortin receptor accessory protein 2 (MRAP2) play important roles in the melanocortin system, and interaction of MC4R and MRAP2 is suggested to play pivotal role in energy balance of vertebrates. Orange-spotted… read more here.
Keywords: mc4r mrap2; mc4r; orange spotted; spotted grouper ... See more keywords
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c02012
Abstract: The melanocortin-4 receptor (MC4R) is a centrally expressed, class A GPCR that plays a key role in the regulation of appetite and food intake. Deficiencies in MC4R signaling result in hyperphagia and increased body mass… read more here.
Keywords: selective mc4r; mc4r; loss; mc4r antagonist ... See more keywords
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b00353
Abstract: The melanocortin receptor 4 (MC4R) subtype of the melanocortin receptor family is a target for therapeutics to ameliorate metabolic dysfunction. Endogenous MC4R agonists possess a critical pharmacophore (HFRW), and cyclization of peptide agonists often enhances… read more here.
Keywords: click chemistry; mc4r; chemistry; melanocortin receptor ... See more keywords
Structural insights into ligand recognition and activation of the melanocortin-4 receptor.
Sign Up to like & getrecommendations! Published in 2021 at "Cell research"
DOI: 10.1038/s41422-021-00552-3
Abstract: Melanocortin-4 receptor (MC4R) plays a central role in the regulation of energy homeostasis. Its high sequence similarity to other MC receptor family members, low agonist selectivity and the lack of structural information concerning MC4R-specific activation… read more here.
Keywords: mc4r; recognition; melanocortin receptor; activation ... See more keywords
Methylphenidate in children with monogenic obesity due to LEPR or MC4R deficiency improves feeling of satiety and reduces BMI‐SDS—A case series
Sign Up to like & getrecommendations! Published in 2019 at "Pediatric Obesity"
DOI: 10.1111/ijpo.12577
Abstract: The clinical phenotype of patients with monogenic obesity due to mutations in the leptin receptor (LEPR) or melanocortin 4 receptor (MC4R) gene is characterized by impaired satiety and hyperphagia, leading to extreme, sometimes life‐threatening weight… read more here.
Keywords: lepr; obesity due; mc4r; satiety ... See more keywords
Pharmacological chaperone action in humanized mouse models of MC4R-linked obesity
Sign Up to like & getrecommendations! Published in 2021 at "JCI Insight"
DOI: 10.1172/jci.insight.132778
Abstract: MC4R mutations represent the largest monogenic cause of obesity, resulting mainly from receptor misfolding and intracellular retention by the cellular quality control system. The present study aimed at determining whether pharmacological chaperones (PCs) that restore… read more here.
Keywords: mouse models; mc4r linked; mc4r; linked obesity ... See more keywords
Rs12970134 near MC4R is associated with appetite and beverage intake in overweight and obese children: A family-based association study in Chinese population
Sign Up to like & getrecommendations! Published in 2017 at "PLoS ONE"
DOI: 10.1371/journal.pone.0177983
Abstract: Background Recent studies indicated that eating behaviors are under genetic influence, and the melanocortin 4 receptor (MC4R) gene polymorphisms can affect the total energy intake and the consumption of fat, protein and carbohydrates. Our study… read more here.
Keywords: rs12970134; intake; mc4r; association ... See more keywords
MC4R Deficiency Causes Dysregulation of Postsynaptic Excitatory Synaptic Transmission as a Crucial Culprit for Obesity.
Sign Up to like & getrecommendations! Published in 2022 at "Diabetes"
DOI: 10.2337/db22-0162
Abstract: Melanocortin-4 receptor (MC4R) in paraventricular nucleus in hypothalamus (PVH) shows bidirectional characterization in modulating food intake and energy homeostasis. Here, we demonstrated that MC4R knock down (MC4R KD) in PVH could attenuate AMPA receptor (AMPAR)… read more here.
Keywords: pvh; mc4r; body weight; mc4r deficiency ... See more keywords
Setmelanotide, a Novel, Selective Melanocortin Receptor-4 Agonist Exerts Anti-inflammatory Actions in Astrocytes and Promotes an Anti-inflammatory Macrophage Phenotype
Sign Up to like & getrecommendations! Published in 2019 at "Frontiers in Immunology"
DOI: 10.3389/fimmu.2019.02312
Abstract: To date, available treatment strategies for multiple sclerosis (MS) are ineffective in preventing or reversing progressive neurologic deterioration, creating a high, and unmet medical need. One potential way to fight MS may be by limiting… read more here.
Keywords: anti inflammatory; phenotype; setmelanotide novel; mc4r ... See more keywords
MRAP2 Interaction with Melanocortin-4 Receptor in SnakeHead (Channa argus)
Sign Up to like & getrecommendations! Published in 2021 at "Biomolecules"
DOI: 10.3390/biom11030481
Abstract: The melanocortin-4 receptor (MC4R) plays an important role in the regulation of food intake and energy expenditure. Melanocortin-2 receptor accessory protein 2 (MRAP2) modulates trafficking, ligand binding, and signaling of MC4R. The Northern snakehead (Channa… read more here.
Keywords: melanocortin receptor; mrap2; snakehead mc4r; mc4r ... See more keywords
A Setmelanotide-like Effect at MC4R Is Achieved by MC4R Dimer Separation
Sign Up to like & getrecommendations! Published in 2022 at "Biomolecules"
DOI: 10.3390/biom12081119
Abstract: Melanocortin 4 receptor (MC4R) is part of the leptin-melanocortin pathway and plays an essential role in mediating energy homeostasis. Mutations in the MC4R are the most frequent monogenic cause for obesity. Due to increasing numbers… read more here.
Keywords: setmelanotide like; homodimerization; mc4r; setmelanotide ... See more keywords