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
Obesity-associated MRAP2 variants impair multiple MC4R-mediated signaling pathways
Sign Up to like & getrecommendations! Published in 2024 at "Human Molecular Genetics"
DOI: 10.1093/hmg/ddaf005
Abstract: The melanocortin-4 receptor (MC4R) is a G protein-coupled receptor expressed at hypothalamic neurons that has an important role in appetite suppression and food intake. Mutations in MC4R are the most common cause of monogenic obesity… read more here.
Keywords: signaling pathways; mc4r mediated; obesity; mc4r ... 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
Abstract 5933: Identifying MC4R-targeted small molecule to investigate MC4R impact on cachexia progression
Sign Up to like & getrecommendations! Published in 2024 at "Cancer Research"
DOI: 10.1158/1538-7445.am2024-5933
Abstract: Background: The melanocortin system participates in energy homeostasis and appetiteregulation. This metabolic system is primarily located in the central nervous system,specifically in the hypothalamus and brainstem region. Within the melanocortin system,there are five established melanocortin… read more here.
Keywords: progression; impact cachexia; mc4r; small molecule ... See more keywords
Abstract Fri094: Increased Ventricular Arrhythmia Burden and Prolong QTc with Preserved Conduction Velocity Hallmark Electrical Heart Disease and Increased Risk of Sudden Death in Melanocortin Type 4 Receptor Knockout Mice
Sign Up to like & getrecommendations! Published in 2025 at "Circulation Research"
DOI: 10.1161/res.137.suppl_1.fri094
Abstract: Background: Obesity (OB) is an independent risk factor for arrhythmias and sudden death (SD) which accounts for ~50% of deaths in OB population, predominantly affecting men (75%). Yet, the mechanisms involved remain poorly defined. We… read more here.
Keywords: mice; risk; mc4r; sudden death ... 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
Hypothalamic POMC neuron-specific knockout of MC4R affects insulin sensitivity by regulating Kir2.1
Sign Up to like & getrecommendations! Published in 2024 at "Molecular Medicine"
DOI: 10.1186/s10020-024-00804-z
Abstract: Imbalance in energy regulation is a major cause of insulin resistance and diabetes. Melanocortin-4 receptor (MC4R) signaling at specific sites in the central nervous system has synergistic but non-overlapping functions. However, the mechanism by which… read more here.
Keywords: mice; pomc neuron; energy; neuron specific ... 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