Article
Endocrinology & Metabolism
Elisabetta Trevellin, Marnie Granzotto, Cristina Host, Francesca Grisan, Diego De Stefani, Alessandro Grinzato, Konstantinos Lefkimmiatis, Claudio Pagano, Rosario Rizzuto, Roberto Vettor
Summary: A novel heterozygous MC4R variant (MC4R-F313Sfs*29) identified in a cohort of 209 obese patients may impair alpha-MSH-induced cAMP and Ca2+ signaling, leading to dysregulation of satiety signaling, hyperphagia, and early onset of obesity.
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM
(2021)
Article
Biochemistry & Molecular Biology
Ren-Lei Ji, Ya-Xiong Tao
Summary: Two new human MRAP2 splice variants were identified in this study, and the effects of MRAP1 and MRAP2 on MC3R and MC4R were investigated. The results suggest that MRAPs play important roles in the signaling and regulation of neural MC3R and MC4R.
Article
Pharmacology & Pharmacy
Didi Zhu, Rui Zhu, Xiaozhu Zhou, Erdan Shi, Xinwei Zhang, Zihao Zhou, Dongcheng Li, Jiangang Zou, Yao Wang
Summary: This study reveals that Epac1 regulates I-Kr, APD, and ERP in guinea pigs with CHF, which may contribute to the proarrhythmic effect of Epac1 in CHF.
CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Ren-Lei Ji, Shan-Shan Jiang, Ya-Xiong Tao
Summary: The neural melanocortin receptors (MCRs) and their accessory proteins MRAP1 and MRAP2 play crucial roles in regulating energy homeostasis. This study reveals that MRAP1 and MRAP2s have species-specific effects on canine neural MCRs, providing a better understanding of their regulation.
Article
Agriculture, Dairy & Animal Science
H. -J. Zhang, Z. -H. Cui, M. Liu, T. -Q. Min, X. Xiao, Z. -Q. Wang, Y. -X. Tao
Summary: The study investigated three naturally occurring mutations in chicken MC3R and found significant defects in receptor pharmacology for G104S and L151R, while the mechanism of action for M54L remains to be further explored.
DOMESTIC ANIMAL ENDOCRINOLOGY
(2021)
Review
Oncology
Gabriel H. Kindl, John A. D'Orazio
Summary: Skin complexion is determined by the amount and type of melanin pigment in the epidermis, with darker skin having more eumelanin for natural sun protection. Understanding pigmentation regulation can lead to strategies for manipulating skin pigmentation to improve UV resistance and reduce skin cancer risk.
PIGMENT CELL & MELANOMA RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Haodong Liu, Xiaojing Li, Penghui Li, Rihan Hai, Jiacheng Li, Qi Fan, Xing Wang, Yujie Chen, Xiaojuan Cao, Xiaoyu Zhang, Ruifeng Gao, Kun Wang, Chenguang Du
Summary: By conducting experiments on mice, it was discovered that VGlut2 neurons in the locus coeruleus play a significant role in weight regulation, while MC4R neurons in the paraventricular nucleus also contribute to weight management. Furthermore, LCVGlut2 neurons exhibit wide-ranging projections, receiving excitatory inputs from multiple brain nuclei. These findings have important implications for the treatment of obesity.
Article
Endocrinology & Metabolism
Rune E. Kuhre, Ida M. Modvig, Sara L. Jepsen, Husun S. Kizilkaya, Cecilie Baech-Laursen, Christopher A. Smith, Frank Reimann, Fiona M. Gribble, Mette M. Rosenkilde, Jens J. Holst
Summary: Studies have shown low expression of MC4R in L-cells of mice and humans, and administration of MC4R agonists did not stimulate GLP-1 secretion in isolated perfused mouse and rat small intestine models. The data suggest that MC4R-activated GLP-1 secretion in rodents may occur exclusively in the colon or involve extra-intestinal signaling.
FRONTIERS IN ENDOCRINOLOGY
(2021)
Article
Immunology
Kiseko Shionoya, Anna Nilsson, Linda Engstrom Ruud, David Engblom, Anders Blomqvist
Summary: Anorexia is a common symptom during infectious and inflammatory disease. The study found that melanocortin-4 receptors (MC4Rs) play an important role in inflammation-induced anorexia. The experiments on mice with transcriptional blockage of the MC4Rs showed that they had the same reduction of food intake following peripheral injection of lipopolysaccharide as wild type mice, but were protected against the anorexic effect of the immune challenge in a test involving olfactory cues. By selectively re-expressing the receptors, it was demonstrated that MC4Rs in the brain stem parabrachial nucleus are responsible for the suppression of food-seeking behavior and also contribute to body weight homeostasis.
BRAIN BEHAVIOR AND IMMUNITY
(2023)
Article
Biochemistry & Molecular Biology
Haolin Mo, Huixia Yu, Yang Li, Timothy P. C. Ezeorba, Zhihao Zhang, Mingxin Yao, Jiajia Yu, Dongmei Xiong, Haixia Liu, Lixin Wang
Summary: This study reports the molecular cloning, tissue distribution, and pharmacological characterization of the grass carp melanocortin-3-receptor (ciMC3R). The ciMC3R mRNA was found to be highly expressed in the brain of grass carp. Four agonists were shown to potentiate the activation of ciMC3R and further increase cAMP production and upregulate the MAPK/ERK signaling. This study provides basic data for exploring the physiological functions of grass carp MC3R, especially in energy homeostasis and food intake.
FISH PHYSIOLOGY AND BIOCHEMISTRY
(2023)
Article
Chemistry, Medicinal
Luis E. Gimenez, Terry A. Noblin, Savannah Y. Williams, Satarupa Mullick Bagchi, Ren-Lei Ji, Ya-Xiong Tao, Claus B. Jeppesen, Kilian W. Conde-Frieboes, Tomi K. Sawyer, Paolo Grieco, Roger D. Cone
Summary: Peptides containing DNal(2 ')7, reported as MC3R subtype-specific agonists, were found to lack MC3R agonist activity. The cell lines used for pharmacological characterization were mischaracterized in terms of receptor subtype expression. Furthermore, peptides containing DNal(2 ')7 primarily exhibit antagonism of MC3R and MC4R.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Neurosciences
Nathan M. Sharfman, Leslie K. Kelley, Maria E. Secci, Nicholas W. Gilpin
Summary: Chronic inflammatory pain is a significant subset of chronic pain diagnoses, affecting a large number of individuals and incurring substantial economic costs. Studies suggest that melanocortin 4 receptors (MC4Rs) may play a role in pain signaling and pain-like behaviors, particularly in the central amygdala (CeA). However, the exact role of MC4Rs in chronic inflammatory pain in males and females is not fully understood.
Article
Immunology
Li Li, Eun-Seon Yoo, Xiujuan Li, Steven C. Wyler, Xiameng Chen, Rong Wan, Amanda G. Arnold, Shari G. Birnbaum, Lin Jia, Jong-Woo Sohn, Chen Liu
Summary: Atypical antipsychotics like risperidone and olanzapine can cause drug-induced metabolic syndrome by inhibiting hypothalamic Mc4r neuronal activity, leading to hyperphagia and weight gain.
JOURNAL OF EXPERIMENTAL MEDICINE
(2021)
Article
Psychiatry
Junfang Zhang, Xinli Guo, Zhangyin Cai, Yan Pan, Hao Yang, Yali Fu, Zixuan Cao, Yaxian Wen, Chao Lei, Chenshan Chu, Yu Yuan, Dongyang Cui, Pengyu Gao, Bin Lai, Ping Zheng
Summary: Chronic morphine administration causes changes in gene expression in different brain regions, potentially contributing to the plasticity associated with addictive behavior. This change in gene expression is most likely mediated by addictive drug-induced epigenetic remodeling of gene expression programs. Previous studies have shown that chronic morphine treatment decreases the levels of miR-105 in the medial prefrontal cortex (mPFC), which is involved in context-induced retrieval of morphine withdrawal memory. However, the mechanism through which chronic morphine treatment decreases miR-105 in the mPFC remains unknown. The present study reveals that chronic morphine induces addiction-related changes in miR-105 in the mPFC through the activation of two transcription factors: CREB, activated by mu receptors-ERK-p90RSK signaling pathway, and glucocorticoid receptor (GR), which acts as a negative transcription factor mediating the decrease in miR-105 levels in the mPFC of rats.
TRANSLATIONAL PSYCHIATRY
(2022)
Article
Biochemistry & Molecular Biology
Gang Xu, Yuan-Yuan Zhang, Gui-Xiang Gu, Guo-Qing Yang, Gong-Yin Ye
Summary: Octopamine is structurally and functionally similar to adrenaline/noradrenaline in vertebrates, but it modulates diverse physiological and behavioral processes in invertebrates. The study cloned beta-adrenergic-like octopamine receptors (CcOct beta Rs) from Cotesia chilonis, revealing varied transcript levels in different tissues and activation by OA and other agonists in heterologous expression. These findings offer important insights into the molecular and pharmacological properties of the receptors in parasitoids.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)