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It has been claimed that the tetrapeptide amide (Phe-Met-Arg-Phe-amide or FMRFamide) has cardioexcitatory properties. The primary amino acid sequence matched that of an earlier identified endogenous opioid peptide, which was generated from the Met-enkephalin precursor. However, a striking diversity and number of -RFamide peptides have also been discovered, indicating that the molluscan peptide is only one member of a large family of neuropeptide transmitters. The precise pattern of biological action depends on the sequence to the NH2-terminal side of the -RFamide moiety, which varies between family members. P518 is a 26 amino acid peptide belonging to the RF(Arg-Phe)amide family that binds to GPR103 with high affinity.

As a leader in membrane protein drug discovery, Creative Biolabs offer a series of peptide P518 family in vitro assays and products with the best quality:

Overview of Peptide P518 Family

26RFa is the endogenous ligands for the mammalian G-protein-coupled receptor QRFPR (GPR103). The cDNAs for GPR103 have been identified in chicken and zebra finch brains. The avian GPR103 sequence has significant similarity to the rat and human GPR103 sequences. By assessing the intracellular Ca2+ content in HEK293T cells transfected with chicken GPR103, the effect of avian 26RFa on GPR103 was examined. The avian brain exhibits widespread expression of the GPR103 gene, with the diencephalon exhibiting the highest levels of mRNA, supporting the idea that GPR103 mediates the orexigenic activity of 26RFa. GPR103 is expressed outside the diencephalic area of the brain in chickens and rats, suggesting that 26RFa has more than just a role in controlling appetite. GPR103 has only been identified in mammals and birds up to this point. To fully understand the 26RFa/GPR103 system's functional importance in fish, amphibians, and reptiles, more research is needed.

 Proposed mechanism of action of 26RFa. Fig.1. Proposed mechanism of action of 26RFa. (Chartrel, 2016)

Peptide P518 Family Drug Discovery

High-affinity ligands for GPR103's G protein-coupled receptor include 26RFa. In mammals, 26RFa participates in a number of crucial biological processes, such as controlling gonadotropin production, controlling food intake, and bone formation. In situations that have undergone thorough research, it is evident that restricting calories also causes an increase in energy expenditure, which results in weight loss. It would be reasonable to assume that -RFamide peptides' actions might similarly follow this trend. If so, the long-ago peptides of the -RFamide family, with their well-preserved effects on food behavior, can serve as effective new therapeutic targets to combat the rise in obesity that has been observed around the world.

Reference

  1. Chartrel, N.; et al. The neuropeptide 26RFa (QRFP) and its role in the regulation of energy homeostasis: a mini-review. Frontiers in Neuroscience. 2016, 10: 549.

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