BACKGROUND AND OBJECTIVE Separate studies have implicated the pedunculopontine tegmental nucleus (PPTg) in processing aversive stimuli to dopamine systems, and melanocortin-4 receptor (MC4R) are broadly expressed by the neurons in the PPTg, but the exact neurosubstrate underlying the regulation of dopamine systems by the central melanocortin pathway is poorly understood. METHODS In this study...

The melanocortin system regulates metabolic homeostasis and inflammation. Melanocortin agonists have contradictorily been reported to both increase and decrease metabolic rate and body temperature. We find two distinct physiologic responses occurring at similar doses. Intraperitoneal administration of the nonselective melanocortin agonist MTII causes a melanocortin-4 receptor (Mc4r)-mediated hy...

Although mutations in the melanocortin-4 receptor (MC4R) gene cause severe early-onset obesity, we still do not have effective approaches to correct the defects of these mutations. Several antagonists have been identified as pharmacoperones of the MC4R whereas no agonist of the MC4R has been reported. In the present study, we investigated the effect of a small molecule agonist of the MC4R, THIQ...

Agouti-related protein (AGRP) is an endogenous antagonist of the melanocortin-4 receptor (MC4R) that functions in the hypothalamic control of feeding behavior. Our previous studies have suggested that in addition to exoloops 2 and 3, several transmembrane domains of MC4R may be important for AGRP binding. However, the detailed molecular basis of MC4R domains in AGRP binding is presently unclear...

melanocortin- 4 receptor (mc4r) and agouti- related peptide (agrp) are involved in energy homeostasis in rats. according to mc4r and agrp effects on luteinizing hormone (lh) secretion, they may influence the estrous cycle of rats. therefore, the aim of this study was to investigate the expression of mc4r and agrp mrnas at different stages of estrous cycle in the rat’s hypothalamus. the estrous ...

The melanocortin-4 receptor (MC4R) plays a critical role in homeostasis and the regulation of body weight. Polymorphisms mc4r gene have been discovered linked to growth, carcass composition, meat quality traits. Therefore, we used CRISPR-Cas9 system target most important freshwater aquaculture species USA, channel catfish, Ictalurus punctatus. Guide RNAs were designed direct Cas9 coding sequenc...

We 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. We have screened libraries of Korean plant extracts and frog peptide analogues in search of MC4R ligan...

More than 70 missense mutations have been identified in the human melanocortin 4 receptor (MC4R), and many of them have been associated with obesity. In a number of cases, the causal link between mutations in MC4R and obesity is controversially discussed. Here, we mined evolution as an additional source of structural information that may help to evaluate the functional relevance of naturally oc...

Genus and Species. Sus scrofa. Locus. Pig Melanocortin-4 Receptor (MC4R) gene. Source and Description of Primers. Primers were designed from well-conserved sequence regions between the human and rat MC4R genes (Genbank accession no. S77415 and U67863, respectively). The primers were used to amplify approximately 760 bp of the porcine MC4R gene from genomic DNA. The sequence of the PCR product s...